分类目录归档：天然产物醌类

天然产物醌类

Doxorubicin hydrochloride(Synonyms: 盐酸阿霉素; Hydroxydaunorubicin hydrochloride)

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天然产物醌类Quinones

Doxorubicin hydrochloride (Synonyms: 盐酸阿霉素; Hydroxydaunorubicin hydrochloride) 纯度: 98.44%

Doxorubicin (Hydroxydaunorubicin) hydrochloride是一种具有细胞毒性的蒽环类抗生素，是一种抗癌化疗试剂。Doxorubicin hydrochloride 是一种有效的人类 DNA topoisomerase I 和 topoisomerase II 抑制剂，IC50 分别为 0.8 μM 和 2.67 μM。Doxorubicin hydrochloride 可降低 AMPK 及其下游靶蛋白乙酰辅酶 A 羧化酶的磷酸化。还可诱导凋亡 (apoptosis) 和自噬。

Doxorubicin hydrochloride(Synonyms: 盐酸阿霉素; Hydroxydaunorubicin hydrochloride)

Doxorubicin hydrochloride Chemical Structure

CAS No. : 25316-40-9

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50 mg ￥900 In-stock
100 mg ￥1600 In-stock
200 mg ￥3000 In-stock
500 mg ￥5000 In-stock
1 g ￥8500 In-stock
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生物活性

Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy[1][2][3].

IC50 & Target[1][2][3]

Topoisomerase II

2.67 μM (IC50)

Daunorubicins/Doxorubicins

 

Topoisomerase I

0.8 μM (IC50)

HIV-1

 

体外研究
(In Vitro)

Doxorubicin hydrochloride (1-8 µM; 24 and 48 hours) decreases the viability of MCF-10F, MCF-7 and MDA-MB-231 cells in a time- and dose-dependent manner[4].
Doxorubicin hydrochloride (1 μM; 3 and 24 hours) results in Hct-116 human colon carcinoma cells reduction in G0/G1 phase and accumulation in G2 phase[5].
Doxorubicin hydrochloride (1 μM for MCF-10F and MDA-MB-231 cells, 4 μM for MCF-7 cells; 48 hours) induces apoptosis by upregulating Bax, caspase-8 and caspase-3 and downregulation of Bcl-2 protein expression[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[4]

Cell Line: Breast cancer cell lines MCF-10F, MCF-7 and MDA-MB-231
Concentration: 0, 1, 2, 4 and 8 μM
Incubation Time: 24 and 48 hours
Result: IC50 was 1 μM for both MCF-10F and MDA-MB-231 cell lines.
IC50 was 4 μM for MCF-7 cell line.

Cell Cycle Analysis[5]

Cell Line: Hct-116 human colon carcinoma cells
Concentration: 1 μM
Incubation Time: 3 hours and 24 hours
Result: Both, bolus (3 h) and continuous (24 h) incubation led to a significant reduction of cells in G0/G1 and accumulation in G2 phase.

Western Blot Analysis[4]

Cell Line: Breast cancer cell lines MCF-10F, MCF-7 and MDA-MB-231
Concentration: 1 μM for MCF-10F and MDA-MB-231 cells, 4 μM for MCF-7 cells
Incubation Time: 48 hours
Result: Bax protein expression was upregulated in MCF-10F and MDA-MB-231 cell lines but MCF-7 cells did not show any significant increase.
Caspase-8 gene expression was upregulated in MCF-10F, but it was downregulated in MCF-7 and MDA-MB-231 cells.

体内研究
(In Vivo)

Treatment with Doxorubicin (2 mg/kg) or Zoledronic acid (100 μg/kg) alone does not statistically significantly decrease final tumor volume compared with saline. Mice treated with Doxorubicin plus Zoledronic acid have statistically significantly smaller final tumor volumes than those treated with Doxorubicin alone[6].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female MF1 nu/nu mice bearing MDA-G8 breast tumor xenograft (6-week-old)[6]
Dosage: Doxorubicin (2 mg/kg); Zoledronic acid (100 μg/kg)
Administration: Intravenous injection; once a week; 6 weeks
Result: Moderate inhibition of subcutaneous tumor growth in mice that were treated with 2 mg/kg Doxorubicin alone or with 100 μg/kg Zoledronic acid alone compared to the saline control.
Mice treated with Zoledronic acid and Doxorubicin together had statistically significant smaller mean tumor volumes on day 42 than those treated with Doxorubicin alone.

Clinical Trial

分子量

579.98

Formula

C27H30ClNO11
CAS 号

25316-40-9
中文名称

盐酸阿霉素；盐酸多柔比星
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 35.71 mg/mL (61.57 mM; ultrasonic and warming and heat to 60°C)

H2O : 20 mg/mL (34.48 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7242 mL 8.6210 mL 17.2420 mL
5 mM 0.3448 mL 1.7242 mL 3.4484 mL
10 mM 0.1724 mL 0.8621 mL 1.7242 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.75 mg/mL (4.74 mM); Clear solution

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. John L. Nitiss, et al. Targeting DNA topoisomerase II in cancer chemotherapy.Nat Rev Cancer. 2009 May;9(5):338-50.

    [2]. Hee-KyungRhee,et al. Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones. Bioorg Med Chem. 2007 Feb 15;15(4):1651-8.

    [3]. P D Foglesong, et al. Doxorubicin inhibits human DNA topoisomerase I. Cancer Chemother Pharmacol. 1992;30(2):123-5.

    [4]. Nesstor Pilco-Ferreto, et al. Influence of doxorubicin on apoptosis and oxidative stress in breast cancer cell lines. Int J Oncol. 2016 Aug;49(2):753-62.

    [5]. Regine Lüpertz, et al. Dose- and time-dependent effects of doxorubicin on cytotoxicity, cell cycle and apoptotic cell death in human colon cancer cells. Toxicology. 2010 May 27;271(3):115-21.

    [6]. Penelope D Ottewell, et al. Antitumor effects of doxorubicin followed by zoledronic acid in a mouse model of breast cancer. J Natl Cancer Inst. 2008 Aug 20;100(16):1167-78.

Shikonin(Synonyms: 紫草素; C.I. 75535; Isoarnebin 4)

发表于由

天然产物醌类Quinones

Shikonin (Synonyms: 紫草素; C.I. 75535; Isoarnebin 4) 纯度: 98.62%

Shikonin 是中草药紫草的主要成分。Shikonin 是一种有效的 TMEM16A 氯化物通道 (chloride channel) 抑制剂，IC50 为 6.5 μM。Shikonin 是一种特异的丙酮酸激酶 M2 (PKM2) 抑制剂，还可以抑制 TNF-α 和 NF-κB途径。Shikonin 通过抑制糖酵解降低外泌体 (exosome) 的分泌。Shikonin 抑制 AIM2炎性体活化。

Shikonin(Synonyms: 紫草素; C.I. 75535; Isoarnebin 4)

Shikonin Chemical Structure

CAS No. : 517-89-5

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生物活性

Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM[1]. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor[2] and can also inhibit TNF-α and NF-κB pathway[3]. Shikonin decreases exosome secretion through the inhibition of glycolysis[4]. Shikonin inhibits AIM2 inflammasome activation[7].

IC50 & Target[1][2][3]

TMEM16A chloride channel

6.5 μM (IC50)

PKM2

 

NF-κB

 

TNF-α

 

体外研究
(In Vitro)

Shikonin is an inhibitor of TMEM16A chloride channel with an IC50 of 6.5 μM[1]. Shikonin is also a specific inhibitor of PKM2[2] and can also inhibit tumor necrosis factor-α (TNF-α) and prevent activation of nuclear factor-κB (NF-κB) pathway. Shikonin at concentrations higher than 50 μM significantly inhibits ormal human keratinocytes (NHKs) viability, compare with that of control (P<0.05). Pretreatment with Shikonin for 2 h attenuates TNF-α-induced NF-κB p65 nuclear translocation[3]. Treatments of Shikonin at 5 and 7.5 μM significantly inhibit the cell viability starting from 12 h and the inhibitory effects are presented in time-dependent patterns compare with the 0 h group in both cell lines. It is found that 5 μM Shikonin displays greater inhibition compare to 2.5 μM at the time points from 24 to 48 h. The invasiveness of U87 and U251 cells is significantly attenuated when treated with Shikonin at 2.5, 5, and 7.5 μM compare with the control group at 24 and 48 h (p<0.01)[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Shikonin significantly inhibits the increase in IL-1β and TNF-α expression levels in the rat model of osteoarthritis, compare with those in the osteoarthritis group (P<0.01). The NF-κB protein expression level is significantly suppressed by Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The induction of the iNOS level is suppressed by treatment with Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The administration of Shikonin markedly weakens the up-regulation of COX-2 protein expression in the rat model of osteoarthritis, as compare with that in the osteoarthritis group (P<0.01). The elevation of caspase-3 activity is significantly reduced by Shikonin treatment in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The downregulation of Akt phosphorylation is also significantly recovered by treatment with Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01)[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

288.30

Formula

C16H16O5
CAS 号
中文名称

紫草素
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (86.72 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4686 mL 17.3430 mL 34.6861 mL
5 mM 0.6937 mL 3.4686 mL 6.9372 mL
10 mM 0.3469 mL 1.7343 mL 3.4686 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 0.5% CMC-Na/saline water

    Solubility: 30 mg/mL (104.06 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.21 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.21 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 4.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
Cell Assay
[4]

U87 and U251 cells are seeded into 96-well plates at a density of 1×104 cells per well in standard DMEM and incubated for 24 h under standard conditions (37°C and 5% CO2). Then the medium is replaced with either blank, serum-free DMEM or DMEM containing Shikonin at concentrations of 2.5, 5, and 7.5 μM. The total volume in each well is 200 μL. Finally, the plates are shaken softly and the optical density is recorded at 570 nm (OD570) using a plate reader. At least three independent experiments are performed[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[5]

Healthy male Sprague-Dawley rats (n=30; 8 to 10-weeks old, 250 to 300 g) are used in this study. Rats are randomly assigned to three groups: Sham-operated group (n=10), osteoarthritis model group (n=10) and Shikonin-treated group (n=10). In the sham-operated group, the right knee joint of the anesthetized rat is only exposed under sterile conditions, and the rats are treated with 0.1 ml/100 g physiological saline (i.p.). In the osteoarthritis model group, osteoarthritis model rats were treated with 0.1 ml/100 g physiological saline (i.p.). In the Shikonin-treated group, osteoarthritis model rats are treated with 10 mg/kg Shikonin (i.p.) once daily for 4 days after osteoarthritis modeling[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Jiang Y et al. Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrhea. Front Pharmacol. 2016 Aug 23;7:270.

    [2]. Li W, et al. Shikonin Suppresses Skin Carcinogenesis via Inhibiting Cell Proliferation. PLoS One. 2015 May 11;10(5):e0126459.

    [3]. Yan Y, et al. Shikonin Promotes Skin Cell Proliferation and Inhibits Nuclear Factor-κB Translocation via Proteasome Inhibition In Vitro. Chin Med J (Engl). 2015 Aug 20;128(16):2228-33.

    [4]. Zhang FY, et al. Shikonin Inhibits the Migration and Invasion of Human Glioblastoma Cells by Targeting Phosphorylated β-Catenin and Phosphorylated PI3K/Akt: A Potential Mechanism for the Anti-Glioma Efficacy of a Traditional Chinese Herbal Medicine. Int J Mol Sci. 2015 Oct 9;16(10):23823-48.

    [5]. Fu D, et al. Shikonin inhibits inflammation and chondrocyte apoptosis by regulation of the PI3K/Akt signaling pathway in a rat model of osteoarthritis. Exp Ther Med. 2016 Oct;12(4):2735-2740.

    [6]. Kathleen M McAndrews, et al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18(1):52.

    [7]. Jernej Zorman, et al. Shikonin Suppresses NLRP3 and AIM2 Inflammasomes by Direct Inhibition of Caspase-1. PLoS One. 2016 Jul 28;11(7):e0159826.

Daunorubicin hydrochloride(Synonyms: 盐酸柔红霉素; Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride)

发表于由

天然产物醌类Quinones

Daunorubicin hydrochloride (Synonyms: 盐酸柔红霉素; Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride) 纯度: 99.23%

Daunorubicin (Daunomycin) hydrochloride 是具有有效抗肿瘤活性的 DNA 拓扑异构酶 II (topoisomerase II)。Daunorubicin 抑制敏感和耐药的埃利氏腹水肿瘤细胞的 DNA 和 RNA 合成。

Daunorubicin hydrochloride(Synonyms: 盐酸柔红霉素; Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride)

Daunorubicin hydrochloride Chemical Structure

CAS No. : 23541-50-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥567 In-stock
10 mg ￥515 In-stock
50 mg ￥1600 In-stock
100 mg ￥2500 In-stock
200 mg ￥3500 In-stock
500 mg ￥7000 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

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生物活性

Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities. Daunorubicin hydrochloride inhibits DNA and RNA synthesis in sensitive and resistant Ehrlich ascites tumor cells.

IC50 & Target[1]

Topoisomerase II

 

Daunorubicins/Doxorubicins

 

体外研究
(In Vitro)

The mean IC50 value is 0.04 μM for Daunorubicin (RP 13057) hydrochloride in Molt-4 cells. Daunorubicin (RP 13057) hydrochloride belongs to the anthracyclines, a group of cytotoxic chemotherapeutics. The cytotoxic effects of anthracyclines are caused by DNA intercalation and the ability to interfere with DNA transcription and replication by inhibiting Topoisomerase II as well as by producing reactive oxygen species[2].
Daunorubicin (RP 13057) hydrochloride inhibits of both DNA and RNA synthesis in HeLa cells over a concentration range of 0.2 through 2 μM. The IC50 value is 0.4 μM for Daunorubicin (RP 13057) hydrochloride in human pancreatic cell line L3.6[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Urinary protein excretion, serum creatinine, and blood urea nitrogen (BUN) level are significantly increased in group Daunorubicin (RP 13057) hydrochloride (3 mg/kg, i.v.) compared with those in group Control. Administration of Daunorubicin (DNR) causes a significant increase in malondialdehyde (MDA) level in renal tissue compared with that in the control group[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

563.98

Formula

C27H30ClNO10
CAS 号

23541-50-6
中文名称

盐酸柔红霉素；盐酸佐柔比星；道诺霉素盐酸盐；盐酸正定霉素；盐酸红比霉素
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (88.66 mM; Need ultrasonic)

H2O : ≥ 34 mg/mL (60.29 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7731 mL 8.8656 mL 17.7311 mL
5 mM 0.3546 mL 1.7731 mL 3.5462 mL
10 mM 0.1773 mL 0.8866 mL 1.7731 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： PBS

    Solubility: 33.33 mg/mL (59.10 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.69 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.69 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Lehmann M, et al. Activity of topoisomerase inhibitors daunorubicin, idarubicin, and aclarubicin in the Drosophila Somatic Mutation and Recombination Test. Environ Mol Mutagen. 2004;43(4):250-7.

    [2]. Svensson SP, et al. Melanin inhibits cytotoxic effects of Doxorubicin and Daunorubicin in MOLT 4 cells. Pigment Cell Res. 2003 Aug;16(4):351-4

    [3]. Gervasoni JE Jr, et al. An effective in vitro antitumor response against human pancreatic carcinoma with paclitaxel and Daunorubicin by induction of both necrosis and apoptosis. Anticancer Res. 2004 Sep-Oct;24(5A):2617-26

    [4]. Arozal W, et al. Telmisartan prevents the progression of renal injury in daunorubicin rats with the alteration of angiotensin II and endothelin-1 receptor expression associated with its PPAR-γ agonist actions. Toxicology. 2011 Jan 11;279(1-3):91-9.

    [5]. Dano K, et al. Inhibition of DNA and RNA synthesis by daunorubicin in sensitive and resistant Ehrlich ascites tumor cells in vitro. Cancer Res. 1972 Jun;32(6):1307-14.
Cell Assay
[2]

The chemosensitivity to Daunorubicin is assessed using the MTT assay. In brief, the 96 well plates are set up with cells at the initial density of 2×105 cells/mL and are incubated at 37°C for 72 h in an atmosphere of 5% CO2 in the absence and presence of nine different concentrations of Daunorubicin (Dnr) or Dox ranging from 1.90 to 0.007 μM in triplicate. After incubation, 10 μL of MTT solution (5 mg/mL tetrazolium salt) is added to each well and the plates are incubated for a further 4 h at 37°C. The formazan salt crystals are dissolved by adding 100 μL 10% SDS in 10 mM HCl solution and incubating over night at 37°C. The absorbance is measured at 540 nm with a reference at 650 nm by a 96-well enzyme-linked immunosorbent assay (ELISA) plate reader. Chemosensitivity is expressed as the IC50, which is the concentration of drug causing 50% cell survival compare to control cells grown without drug. Calculations are carried out using Microsoft Excel[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

Rat[4]
Eight-week-old male Sprague-Dawley rats are used. The animals are quarantined and acclimatized for the additional 2 weeks prior to the initiation of the experiments. On day 0, each animal receives a single intravenous injection of Daunorubicin at a dose of 3 mg/kg (i.v.). Daunorubicin is administered in three equal injections at 48 h intervals for a period of one week to achieve an accumulative dose of 9 mg/kg, which is well documented to produce cardiotoxicity and nephrotoxicity. Age-matched rats are injected with corresponding volumes of 0.9% NaCl and used as a control (group Control;n=5). Twenty-two DNR-treated rats are randomly divided into two groups and received oral administration of Telmisartan (10 mg/kg/day; group Daunorubicin+Telmisartan; n=10) or vehicle (group Daunorubicin; n=12). The dose of Telmisartan is chosen on the basis of a previous report. Administration of Telmisartan is started on the same day as Daunorubicin administration and continued for 5 additional weeks after cessation of Daunorubicin administration (6 weeks total period). This duration of study is chosen on the basis of previous reports. On day 41, rats are placed individually in metabolic cages for 24-h urine collections for the measurement of protein concentrations and body weight (BW) is measured. After the end of the study period (6 weeks), rats are sacrificed and kidney tissue is harvested for semi-quantitative immunoblotting and immunohistochemical studies.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Lehmann M, et al. Activity of topoisomerase inhibitors daunorubicin, idarubicin, and aclarubicin in the Drosophila Somatic Mutation and Recombination Test. Environ Mol Mutagen. 2004;43(4):250-7.

    [2]. Svensson SP, et al. Melanin inhibits cytotoxic effects of Doxorubicin and Daunorubicin in MOLT 4 cells. Pigment Cell Res. 2003 Aug;16(4):351-4

    [3]. Gervasoni JE Jr, et al. An effective in vitro antitumor response against human pancreatic carcinoma with paclitaxel and Daunorubicin by induction of both necrosis and apoptosis. Anticancer Res. 2004 Sep-Oct;24(5A):2617-26

    [4]. Arozal W, et al. Telmisartan prevents the progression of renal injury in daunorubicin rats with the alteration of angiotensin II and endothelin-1 receptor expression associated with its PPAR-γ agonist actions. Toxicology. 2011 Jan 11;279(1-3):91-9.

    [5]. Dano K, et al. Inhibition of DNA and RNA synthesis by daunorubicin in sensitive and resistant Ehrlich ascites tumor cells in vitro. Cancer Res. 1972 Jun;32(6):1307-14.

Geldanamycin(Synonyms: 格尔德霉素)

发表于由

天然产物醌类Quinones

Geldanamycin (Synonyms: 格尔德霉素) 纯度: 99.78%

Geldanamycin是 Hsp90 抑制剂，具有抗许多革兰氏阳性和一些革兰氏阴性细菌的活性。Geldanamycin 还具有抗流感病毒 H5N1 的活性。

Geldanamycin(Synonyms: 格尔德霉素)

Geldanamycin Chemical Structure

CAS No. : 30562-34-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1544 In-stock
5 mg ￥1252 In-stock
10 mg ￥1989 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Geldanamycin 相关产品

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  • Antibiotics Library
  • Microbial Metabolite Library

生物活性

Geldanamycin is a Hsp90 inhibitor with antimicrobial activity against many Gram-positive and some Gram-negative bacteria. Geldanamycin has anti-influenza virus H5N1 activities.

IC50 & Target

HSP90

1.2 μM (Kd)

体外研究
(In Vitro)

Geldanamycin significantly delays and reduces viperin expression, indicating that IRF3 is involved in viperin induction in RAW264.7 cells[1]. Geldanamycin (GA), a benzoquinone ansamycin, protected against neuronal injury induced by oxygen-glucose deprivation (OGD)/zVAD treatment in cultured primary neurons. More importantly, Geldanamycin decreases RIP1 protein level in a time and concentration-dependent manner. Geldanamycin also decreases the Hsp90 protein level, which causes instability of RIP1 protein, resulting in decreased RIP1 protein level but not RIP1 mRNA level after Geldanamycin treatment[2]. Geldanamycin (GA) is identified as the first natural product inhibitor of Hsp90 that binds to the N-terminal ATPase domain of Hsp90 to inhibit its chaperone function, and significantly induces tumor cell death via an apoptotic mechanism[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

560.64

Formula

C29H40N2O9
CAS 号

30562-34-6
中文名称

格尔德霉素
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (89.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7837 mL 8.9184 mL 17.8368 mL
5 mM 0.3567 mL 1.7837 mL 3.5674 mL
10 mM 0.1784 mL 0.8918 mL 1.7837 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (4.46 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.46 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.46 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.46 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Tang HB, et al. Viperin inhibits rabies virus replication via reduced cholesterol and sphingomyelin and is regulated upstream by TLR4. Sci Rep. 2016 Jul 26;6:30529

    [2]. Chen WW, et al. RIP1 mediates the protection of Geldanamycin on neuronal injury induced by oxygen-glucosedeprivation combined with zVAD in primary cortical neurons. J Neurochem. 2012 Jan;120(1):70-7.

    [3]. Lin Z, et al. 17-ABAG, a novel Geldanamycin derivative, inhibits LNCaP-cell proliferation through heat shock protein 90 inhibition. Int J Mol Med. 2015 Aug;36(2):424-32.

    [4]. Roe SM, et al. Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin. J Med Chem. 1999 Jan 28;42(2):260-6.

    [5]. Wang C, et al. Geldanamycin Reduces Acute Respiratory Distress Syndrome and Promotes the Survival of Mice Infected with the Highly Virulent H5N1 Influenza Virus. Front Cell Infect Microbiol. 2017 Jun 15;7:267.

Emodin(Synonyms: 大黄素; Frangula emodin)

发表于由

天然产物醌类Quinones

Emodin (Synonyms: 大黄素; Frangula emodin) 纯度: 99.39%

Emodin (Frangula emodin) 是一种蒽醌衍生物，是一种抗 SARS-CoV 化合物。Emodin 阻断 SARS 冠状病毒刺突蛋白和血管紧张素转化酶 2 (ACE2) 的相互作用。Emodin 抑制酪蛋白激酶 2 (CK2)。 具有抗炎和抗癌作用。Emodin 还是一种有效的选择性 11β-HSD1 抑制剂，对人和小鼠 11β-HSD1 的 IC50 分别为 186 和 86 nM。Emodin 可改善饮食诱导的肥胖小鼠的代谢紊乱。

Emodin(Synonyms: 大黄素; Frangula emodin)

Emodin Chemical Structure

CAS No. : 518-82-1

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥385 In-stock
50 mg ￥350 In-stock
100 mg ￥560 In-stock
200 mg ￥1000 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

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生物活性

Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].

IC50 & Target[1][2][3]

SARS-CoV

 

CK2α Wild-type

1.4 μM (IC50, at ATP concentration is 10 μM)

CK2α Wild-type

5.9 μM (IC50, at ATP concentration is 50 μM)

mouse 11β-HSD1

86 nM (IC50)

human 11β-HSD1

186 nM (IC50)

体外研究
(In Vitro)

Emodin (10-400 μM) blocks the binding of S protein to ACE2 in a dose-dependent manner with the IC50 value of 200 μM[1].
Emodin (5-50 μM) inhibits the S protein-pseudotyped retrovirus infectivity in a dose-dependent manner. Emodin blocks the SARS-CoV S protein binding to Vero E6 cells[1].
Emodin inhibits casein kinase-2 (CK2) with IC50s of 5.9, 30.0, and 7.1 μM for CK2α Wild-type, Ile174Ala mutant, and His160Ala mutant at ATP concentration is 50 μM, respectively. The IC50s are 1.40 and 38.00 μM for CK2α Wild-type, and Val66Ala mutant at ATP concentration is 10 μM[2].
Emodin exhibits low inhibitory activity against mouse and human 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), with an IC50 higher than 1 mM, indicating that Emodin is more than 5000-fold selective for the human and mouse 11β-HSD1 enzymes over the type 2 isoenzyme[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Vero E6 cells transfected with the plasmid encoding ACE2
Concentration: 0, 5, 25, 50 μM
Incubation Time: 24 hours
Result: Vero cells treated with 50 μM remained 82.4±3.8% viability, the anti-SARS-CoV activity was not due to toxicity.

体内研究
(In Vivo)

Emodin (single oral administration of 100 or 200 mg/kg) inhibits 11β-HSD1 activity in normal C57BL/6J male mice[3].
Emodin (100 mg/kg; oral administration; b.i.d.) improves insulin sensitivity and lipid metabolism, and lowers blood glucose and hepatic PEPCK, and glucose-6-phosphatase mRNA in diet-induced obese (DIO) mice[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J male mice[3]
Dosage: 100 or 200 mg/kg
Administration: Acute administered p.o. ; Two hours later, the mice were killed by cervical dislocation,
Result: Significantly inhibited liver 11β-HSD1 enzymatic activity by 17.6 and 31.3% and mesenteric fat 11β-HSD1 enzymatic activity by 21.5 and 46.7% at 100 or 200 mg/kg, respectively.
Animal Model: DIO mice (C57BL/6J male mice were fed a formulated research diet)[3]
Dosage: 100 mg/kg
Administration: Oral gavage; twice per day; for 35 days
Result: Reduced fasting glucose concentrations to 77.2% of the vehicle control mice after 7 days of treatment, and these remained significantly lower throughout the treatment period.
Exhibited a significant reduction in blood glucose levels at all time-points following oral glucose challenge after 24 days of treatment.
Evoked a significantly greater reduction in blood glucose values 40 and 90 min after insulin injection after 28 days of treatment.
The serum insulin level was also significantly reduced, to 66.2% of control mice, after 35 days of treatment.
Improved the lipid profiles. The serum triglyceride and total cholesterol levels were significantly reduced by 19.3 and 12.5% after 35 days of treatment, respectively.
Caused a 22.7% reduction of non-esterified free fatty acid (NEFA) level.
Lowered body weight and appetite from day 18 of the treatment; their body weights were reduced by 13.9% at the end of treatment.

Clinical Trial

分子量

270.24

Formula

C15H10O5
CAS 号

518-82-1
中文名称

大黄素
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

Acetone : 10.87 mg/mL (40.22 mM; Need ultrasonic)

DMSO : 5.41 mg/mL (20.02 mM; Need ultrasonic)

Ethanol : < 1 mg/mL (ultrasonic) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7004 mL 18.5021 mL 37.0041 mL
5 mM 0.7401 mL 3.7004 mL 7.4008 mL
10 mM 0.3700 mL 1.8502 mL 3.7004 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 0.5% MC  0.5% Tween-80

    Solubility: 10 mg/mL (37.00 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 0.5% CMC-Na/saline water

    Solubility: 3.33 mg/mL (12.32 mM); Suspened solution; Need ultrasonic

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Tin-Yun Ho, et al. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 interaction. Antiviral Res. 2007 May;74(2):92-101.

    [2]. Stefania Sarno, et al. Toward the rational design of protein kinase casein kinase-2 inhibitors. Pharmacol Ther. Feb-Mar 2002;93(2-3):159-68.

    [3]. Ying Feng, et al. Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice. Br J Pharmacol. 2010 Sep;161(1):113-26.

Menadione(Synonyms: 维生素K3; Vitamin K3)

发表于由

天然产物醌类Quinones

Menadione (Synonyms: 维生素K3; Vitamin K3) 纯度: 98.07%

Menadione是合成的萘醌，可在体内转化为活性维生素K2。

Menadione(Synonyms: 维生素K3; Vitamin K3)

Menadione Chemical Structure

CAS No. : 58-27-5

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1 g ￥650 In-stock
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生物活性

Menadione, a synthetic naphthoquinone, can be converted to active vitamin K2 in vivo. Target: Others Menadione (Vitamin K3) is a synthetic analogue of of 1,4-naphthoquinone with a methyl group in the 2-position. Menadione is used as a phosphatase inhibitor and an inhibitor of mitochondrial DNA polymerase γ (pol γ). Menadione can be used as an oxidative injury (free radical generator) inducing agent [1].

IC50 & Target

Human Endogenous Metabolite

 

Clinical Trial

分子量

172.18

Formula

C11H8O2
CAS 号

58-27-5
中文名称

甲萘醌；维生素K3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (290.39 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.8079 mL 29.0394 mL 58.0788 mL
5 mM 1.1616 mL 5.8079 mL 11.6158 mL
10 mM 0.5808 mL 2.9039 mL 5.8079 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (12.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (12.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (12.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (12.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (12.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (12.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. http://en.wikipedia.org/wiki/Menadione

Cryptotanshinone(Synonyms: 隐丹参酮; Cryptotanshinon; Tanshinone c)

发表于由

天然产物醌类Quinones

Cryptotanshinone (Synonyms: 隐丹参酮; Cryptotanshinon; Tanshinone c) 纯度: 98.46%

Cryptotanshinone是从丹参的根中提取的天然化合物，具有抗肿瘤活性。 Cryptotanshinone抑制 STAT3 的 IC50 为4.6 μM。

Cryptotanshinone(Synonyms: 隐丹参酮; Cryptotanshinon; Tanshinone c)

Cryptotanshinone Chemical Structure

CAS No. : 35825-57-1

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Free Sample (0.1-0.5 mg)   Apply now  
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50 mg ￥950 In-stock
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200 mg   询价  

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生物活性

Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.

IC50 & Target[1]

STAT3

4.6 μM (IC50)

体外研究
(In Vitro)

Cryptotanshinone significantly inhibits STAT3-dependent luciferase activity, the STAT3 Tyr705 phosphorylation and the dimerization of STAT3, compared to tanshinone IIA which exhibits no activity. Cryptotanshinone (7 μM) dramatically blocks STAT3 Tyr705 phosphorylation but not STAT3 Ser727 phosphorylation in DU145 cells, and significantly inhibits JAK2 phosphorylation with IC50 of appr 5 μM without affecting the phosphorylation of upstream kinases c-Src and EGFR, suggesting the inhibition of STAT3 Tyr705 phosphorylation might due to a direct mechanism probably by binding to the SH2 domain of STAT3. Cryptotanshinone significantly inhibits the proliferation of DU145 prostate cancer cells harboring constitutively active STAT3 with GI50 of 7 μM by blocking STAT3 activity, which leads to the down-regulation of cyclin D1, Bcl-xL, and survivin, subsequently the accumulation in the G0-G1 phase. Cryptotanshinone exhibits less growth inhibitory effect on PC3, LNCaP and MDA-MB-468 cells[1]. Cryptotanshinone significantly attenuates the in vitro hormonal effects of DEX on ovaries, as indicated by a significant decrease in T and an increase in P levels in the culture medium. Cryptotanshinone significantly increases the levels of phosphorylated AKT2 and GSK3β in the DEX-treated ovaries[2]. Cotreatment with imatinib and Cryptotanshinone shows a significant synergistic killing effect in both imatinib sensitive and resistant CML cell lines, as well as primary CML cells[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Cryptotanshinone reverses the ovarian IR and significantly increases 2-deoxy-D-[1,2-3H]-glucose uptake in all examined tissues from the DEX-treated mice. Cryptotanshinone significantly reduces the ovulation rate and plasma E2 and P levels[2]. Cryptotanshinone administration significantly reduces the body weight and food intake of ob/ob mice (C57BL/6J-Lepob) and diet-induced obese (DIO) mice in a dose-dependent manner. Cryptotanshinone causes noticeably less fat in the adipose tissues, significant reductions of serum triglycerides and cholesterol levels, and 2.5- to 3-fold higher AMPK activity of the skeletal muscles than in the control mice. Oral administration of Cryptotanshinone at 600 mg/kg/day produces dramatic reductions in blood glucose levels of ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb), and ZDF rats, which occur after 3 days and persist over the entirety of the monitoring period[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

296.36

Formula

C19H20O3
CAS 号

35825-57-1
中文名称

隐丹参酮；隐丹参醌；丹参酮 C
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (16.87 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3743 mL 16.8714 mL 33.7427 mL
5 mM 0.6749 mL 3.3743 mL 6.7485 mL
10 mM 0.3374 mL 1.6871 mL 3.3743 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 0.83 mg/mL (2.80 mM); Suspended solution; Need ultrasonic

    此方案可获得 0.83 mg/mL (2.80 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.83 mg/mL (2.80 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.80 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.83 mg/mL (2.80 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Shin DS, et al. Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells. Cancer Res. 2009 Jan 1;69(1):193-202.

    [2]. Huang Y, et al. Cryptotanshinone reverses ovarian insulin resistance in mice through activation of insulin signaling and the regulation of glucose transporters and hormone synthesizing enzymes. Fertil Steril. 2014 Aug;102(2):589-596.e4.

    [3]. Ge Y, et al. Cryptotanshinone acts synergistically with imatinib to induce apoptosis of human chronic myeloid leukemia cells. Leuk Lymphoma. 2014 Jun 25:1-9.

    [4]. Kim EJ, et al. Antidiabetes and antiobesity effect of cryptotanshinone via activation of AMP-activated protein kinase. Mol Pharmacol. 2007 Jul;72(1):62-72. Epub 2007 Apr 11.
Kinase Assay
[1]

HCT-116 cells are transiently transfected with reporter plasmid having the STAT3-binding element for regulating luciferase assay. Cells are treated with Cryptotanshinone for 24 hours at a concentration range of 0.2 to 50 μM. After treatment, cells are harvested in 20 μL of passive lysis buffer and luciferase activity is evaluated by the Dual Luciferase Reporter Assay kit on Wallac Victor2. The concentration of Cryptotanshinone that inhibits the luciferase activity by 50% represents IC50 value.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[3]

The MTT assay is used for the assessment of cell growth inhibition as described previously. Cells are seeded at a density of 8000 cells per well in 96-well plates in RPMI-1640 containing 10% FBS. Different concentrations of imatinib and CPT are added and incubated for another 24 h. Then, 20 μL of MTT are added into each well and the absorbance at 570 nm is measured on an enzyme linked immunosorbent assay (ELISA) plate reader. The coefficient of drug interaction (CDI) between imatinib and CPT is determined according to a previous study. The calculated method is as follows: CDI/AB/(A × B). According to the absorbance of each group, AB is the ratio of the combination group to the control group; A or B is the ratio of the single agent group to the control group. CDI < 1 indicates a synergistic effect; CDI=1 indicates an additive effect; CDI > 1 indicates an antagonistic effect. In the combination treatment group, the concentrations of CPT are arbitrarily designated according to the 50% inhibitory concentration (IC50) value. Then, the cell viabilities are determined after treatment with different concentrations of imatinib plus CPT (constant CPT concentration for one cell type). Finally, the combination IC50 values of imatinib are calculated, and are represented in Table I. The primary CML cells CP1 to CP3 are isolated from patients in chronic phase, while BC1 and BC2 are isolated from patients in blast crisis. Three independent sets of experiments are performed. The IC50 values are presented as the mean±standard deviation (SD).

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Shin DS, et al. Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells. Cancer Res. 2009 Jan 1;69(1):193-202.

    [2]. Huang Y, et al. Cryptotanshinone reverses ovarian insulin resistance in mice through activation of insulin signaling and the regulation of glucose transporters and hormone synthesizing enzymes. Fertil Steril. 2014 Aug;102(2):589-596.e4.

    [3]. Ge Y, et al. Cryptotanshinone acts synergistically with imatinib to induce apoptosis of human chronic myeloid leukemia cells. Leuk Lymphoma. 2014 Jun 25:1-9.

    [4]. Kim EJ, et al. Antidiabetes and antiobesity effect of cryptotanshinone via activation of AMP-activated protein kinase. Mol Pharmacol. 2007 Jul;72(1):62-72. Epub 2007 Apr 11.

Coenzyme Q10(Synonyms: 辅酶Q10; CoQ10; Ubiquinone-10)

发表于由

天然产物醌类Quinones

Coenzyme Q10 (Synonyms: 辅酶Q10; CoQ10; Ubiquinone-10) 纯度: ≥98.0%

Coenzyme Q10是电子传递链的重要辅助因子，也是一种有效的抗氧化剂。

Coenzyme Q10(Synonyms: 辅酶Q10; CoQ10; Ubiquinone-10)

Coenzyme Q10 Chemical Structure

CAS No. : 303-98-0

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
100 mg ￥450 In-stock
200 mg ￥650 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Coenzyme Q10 相关产品

•相关化合物库:

  • Natural Product Library Plus
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生物活性

Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Coenzyme Q10 is an obligatory member of the respiratory chain in the mitochondria of all cells. Therefore, it is an essential ingredient in the formation of adenosine triphosphate (ATP), the source of energy in most cellular processes. Coenzyme Q10 is located in the mitochondria, lysosomes, and Golgi and plasma membranes, and provides an antioxidant action either by direct reaction with free radicals or by regeneration of tocopherol and ascorbate from their oxidised state[1]. Coenzyme Q10 is a popular dietary supplement because of its recognition by the public as an important nutrient in supporting human health. The rationale for the use of Coenzyme Q10 as a therapeutic agent in several cardiovascular and degenerative neurologic and neuromuscular diseases is based upon its fundamental role in mitochondrial function and cellular bioenergetics[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Because of its hydrophobicity and large molecular weight, absorption of dietary Coenzyme Q10 is slow and limited. In the case of dietary supplements, solubilized Coenzyme Q10 formulations show enhanced bioavailability. The Tmax is around 6 h, with an elimination half-life of about 33 h. The reference intervals for plasma Coenzyme Q10 range from 0.40 to 1.91 mM in healthy subjects. With Coenzyme Q10 supplements there is reasonable correlation between increase in plasma Coenzyme Q10 and ingested dose up to a certain point. Animal data show that Coenzyme Q10 in large doses is taken up by all tissues including heart and brain mitochondria[2]. In 12-month-old rats administration of coenzyme Q10 results in significant increases in cerebral cortex mitochondrial concentrations of coenzyme Q10. Oral administration of coenzyme Q10 markedly attenuates striatal lesions produced by systemic administration of 3-nitropropionic acid and significantly increases life span in a transgenic mouse model of familial amyotrophic lateral sclerosis[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

863.34

Formula

C59H90O4
CAS 号

303-98-0
中文名称

辅酶Q10
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture and light

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据
In Vitro: 

DMF : 40 mg/mL (46.33 mM; Need ultrasonic)

Ethanol : 2.5 mg/mL (2.90 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1583 mL 5.7915 mL 11.5829 mL
5 mM 0.2317 mL 1.1583 mL 2.3166 mL
10 mM 0.1158 mL 0.5791 mL 1.1583 mL

*

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMF    90% (20% SBE-β-CD in saline)

    Solubility: 3 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Yang YK, et al. Coenzyme Q10 treatment of cardiovascular disorders of ageing including heart failure, hypertension and endothelial dysfunction. Clin Chim Acta. 2015 Oct 23;450:83-9.

    [2]. Bhagavan HN, et al. Coenzyme Q10: absorption, tissue uptake, metabolism and pharmacokinetics. Free Radic Res. 2006 May;40(5):445-53.

    [3]. Matthews RT, et al. Coenzyme Q10 administration increases brain mitochondrial concentrations and exerts neuroprotective effects. Proc Natl Acad Sci U S A. 1998 Jul 21;95(15):8892-7.
Animal Administration
[3]

Rats[3]

The effects of oral administration of coenzyme Q10 on 3-NP-induced striatal lesions are examined in 300- to 350-g rats (n=5-10). Animals receive either rat chow supplemented with coenzyme Q10 at 200 mg/kg or unsupplemented rat chow. After 1 week they are treated with 3-NP at a dose of 10 mgykg i.p. twice a day until either a control or treated animal became symptomatic with hindlimb dystonia, and then sacrificed in pairs[3].

Mice[3]

To determine whether coenzyme Q10 exerts neuroprotective effects in a transgenic mouse model of a human neurodegenerative disorder, coenzyme Q10 (200 mg/kg) is administered orally to 16 transgenic mice overexpressing a human CuyZn superoxide dismutase (SOD1) mutation, as compared with 13 animals that receive unsupplemented rat chow. The mice used are the G1 line, which expresses high levels of human SOD with the G93A mutation. Treatment is started at 50 days after birth. Treatment is continued until mice reach end-stage disease[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Yang YK, et al. Coenzyme Q10 treatment of cardiovascular disorders of ageing including heart failure, hypertension and endothelial dysfunction. Clin Chim Acta. 2015 Oct 23;450:83-9.

    [2]. Bhagavan HN, et al. Coenzyme Q10: absorption, tissue uptake, metabolism and pharmacokinetics. Free Radic Res. 2006 May;40(5):445-53.

    [3]. Matthews RT, et al. Coenzyme Q10 administration increases brain mitochondrial concentrations and exerts neuroprotective effects. Proc Natl Acad Sci U S A. 1998 Jul 21;95(15):8892-7.

β-Lapachone(Synonyms: ARQ-501; NSC-26326)

发表于由

天然产物醌类Quinones

β-Lapachone (Synonyms: ARQ-501; NSC-26326) 纯度: 99.85%

β-Lapachone (ARQ-501;NSC-26326) 是一种天然的萘醌类化合物，是拓扑异构酶 I (topoisomerase I) 抑制剂，通过抑制细胞周期进程来诱导细胞凋亡。

β-Lapachone(Synonyms: ARQ-501; NSC-26326)

β-Lapachone Chemical Structure

CAS No. : 4707-32-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in Ethanol ￥660 In-stock
10 mg ￥600 In-stock
50 mg ￥2100 In-stock
100 mg ￥3900 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.

IC50 & Target[1]

Topoisomerase I

 

体外研究
(In Vitro)

β-Lapachone is a topoisomerase I inhibitor. β-Lapachone (25 μM) inhibits camptothecin-induced DNA cleavage[1]. β-Lapachone (10-40 μM) significantly reduces the colony-forming ability of CHO cells, and is cytotoxic in S phase. β-Lapachone at above 10 μM, causes a heavy DNA-strand breaks in CHO cells[2]. β-Lapachone (10 μM) suppresses JCPyV replication in IMR-32 cells. β-Lapachone (1.0 µM) potently affects JCPyV propagation in JCI cells. β-Lapachone (0.01-0.1 μM) inhibits VP1 production in JCI cells[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

β-Lapachone (0.066%) ameliorates cisplatin-induced renal injury and when in combination with cisplatin, the affect is more significant in mice. β-Lapachone increases Mre11-Rad50-Nbs1 (MRN) complex expression in mice[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

242.27

Formula

C15H14O3
CAS 号

4707-32-8
中文名称

β-拉帕醌
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (103.19 mM; Need ultrasonic)

Ethanol : 8.33 mg/mL (34.38 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1276 mL 20.6381 mL 41.2763 mL
5 mM 0.8255 mL 4.1276 mL 8.2553 mL
10 mM 0.4128 mL 2.0638 mL 4.1276 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.32 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.32 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.32 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Li CJ, et al. beta-Lapachone, a novel DNA topoisomerase I inhibitor with a mode of action different from camptothecin. J Biol Chem. 1993 Oct 25;268(30):22463-8.

    [2]. Vanni A, et al. DNA damage and cytotoxicity induced by beta-lapachone: relation to poly(ADP-ribose) polymerase inhibition. Mutat Res. 1998 Jun 5;401(1-2):55-63.

    [3]. Kim TW, et al. β-Lapachone enhances Mre11-Rad50-Nbs1 complex expression in cisplatin-induced nephrotoxicity. Pharmacol Rep. 2016 Feb;68(1):27-31.
Kinase Assay
[1]

DNA topoisomerase I is incubated in the presence or absence of drugs (including β-Lapachone), in 20 μL of relaxation buffer (50 mM Tris (pH 7.5). 50 mM KCl, 10 mM MgCl2, 0.5 mM dithiothreitol, 0.5 mM EDTA, 30 μg/mL bovine serum albumin) for 30 min at 37°C. Reactions are stopped by adding 1% SDS and proteinase K (50 μg/mL). After an additional 1-h incubation at 37°C, the products are separated by electrophoresis in 1% agarose gel in TAE buffer (0.04 M tris acetate, 0.001 M EDTA). The gel is stained with ethidium bromide after electrophoresis. The photographic negative is scanned with an NIH image analysis system[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[4]

Cytotoxicity is measured by an MTT assay. IMR-32 and JCI cells are plated in 96-well microtiter plates at a concentration of 5.0 × 104 (topotecan) or 2.5 × 104 (β-lapachone) cells/well/100 µL medium 24 hr prior to addition of various concentrations of topotecan or β-lapachone. The cells are then incubated for 72 hr at 37°C in a CO2 incubator. Cell proliferation is assessed using a Cell Proliferation Kit I. Experiments are performed using four independent cultures[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Male Balb/c mice are provided a commercial pellet diet and water ad libitum. After 1 week of acclimation, the mice are randomly allocated to one of the following groups (5 per group): control, β-lapachone, cisplatin (18 mg/kg, ip), and β-lapachone + cisplatin (18 mg/kg, ip). The β-lapachone groups are fed a diet containing the drug (0.066) for 2 weeks prior to cisplatin injection. All mice are sacrificed under carbon dioxide anesthesia 3 days after cisplatin injection. The blood samples are subjected to serum BUN and CRE analyses. Half of the kidney is quickly removed for histopathological and immunohistochemical (IHC) studies. The other half is stored at −70°C until western blot assay[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Li CJ, et al. beta-Lapachone, a novel DNA topoisomerase I inhibitor with a mode of action different from camptothecin. J Biol Chem. 1993 Oct 25;268(30):22463-8.

    [2]. Vanni A, et al. DNA damage and cytotoxicity induced by beta-lapachone: relation to poly(ADP-ribose) polymerase inhibition. Mutat Res. 1998 Jun 5;401(1-2):55-63.

    [3]. Kim TW, et al. β-Lapachone enhances Mre11-Rad50-Nbs1 complex expression in cisplatin-induced nephrotoxicity. Pharmacol Rep. 2016 Feb;68(1):27-31.

Rhein(Synonyms: 大黄酸; Rheic Acid; Rhubarb yellow; Monorhein)

发表于由

天然产物醌类Quinones

Rhein (Synonyms: 大黄酸; Rheic Acid; Rhubarb yellow; Monorhein) 纯度: 99.73%

Rhein 是一种蒽醌类化合物，具有抗炎、抗氧化、抗癌等作用。

Rhein(Synonyms: 大黄酸; Rheic Acid; Rhubarb yellow; Monorhein)

Rhein Chemical Structure

CAS No. : 478-43-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550 In-stock
100 mg ￥500 In-stock
200 mg ￥800 In-stock
500 mg ￥1600 In-stock
1 g   询价  
5 g   询价  

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生物活性

Rhein is a lipophilic anthraquinone extensively found in medicinal herbs, and has many pharmacological effects, including epatoprotective, nephroprotective, anti-inflammatory, antioxidant, anticancer, and antimicrobial activities. IC50 value: Target: In vitro: Rhein (0.1 and 1 mg/mL) evidently suppressed cell proliferation and mitogen-activated protein (MAP) kinase activation in human colon adenocarcinoma cells (Caco-2) but significantly lessened H2O2-induced DNA damage and the elevated MDA and ROS levels induced by H2O2/Fe2+ at the concentrations of 0.1–10 mg/mL [1]. In vivo: Oral administration of rhein (150 mg/kg/d) evidently ameliorated renal interstitial fibrotic lesions and attenuated the expression of α-SMA and deposition of fibronectin (FN) in mice with renal interstitial fibrosis induced by unilateral ureteral obstruction. Rhein also suppressed TGF-β1 and its type I receptor expression in obstructed kidneys [1]. The biochemical parameters results of IgAN model rats showed that rhein-prevented and rhein-treated both improved the biochemical parameters and relieved renal pathological injury. The expressions of renal tissue TLR4, TGF-β1, but not TLR9 were significantly elevated in IgAN model rats (P < 0.05). Rhein-prevented and rhein-treated both inhibited TLR4 and TGF-β1 expressions [2].

分子量

284.22

Formula

C15H8O6
CAS 号

478-43-3
中文名称

大黄酸
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 12.17 mg/mL (42.82 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5184 mL 17.5920 mL 35.1840 mL
5 mM 0.7037 mL 3.5184 mL 7.0368 mL
10 mM 0.3518 mL 1.7592 mL 3.5184 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Xiaowen Chen, et al. Toll-like receptor 4 is involved in a protective effect of rhein on immunoglobulin A nephropathy. Indian J Pharmacol. 2015 Jan-Feb; 47(1): 27–33.

    [2]. Hou ML, et al. The Drug-Drug Effects of Rhein on the Pharmacokinetics and Pharmacodynamics of Clozapine in Rat Brain Extracellular Fluid by In Vivo Microdialysis. J Pharmacol Exp Ther. 2015 Oct;355(1):125-34.

    [3]. Yan-Xi Zhou, et al. Rhein: A Review of Pharmacological Activities. Evid Based Complement Alternat Med. 2015; 2015: 578107.