标签归档：雷公藤

Wilfortrine(Synonyms: 雷公藤春碱)

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Wilfortrine (Synonyms: 雷公藤春碱)

Wilfortrine 是一种生物活性倍半萜生物碱。Wilfortrine 表现出免疫抑制作用。Wilfortrine 还可以抑制小鼠白血病细胞的生长，并具有抗 HIV 活性。

Wilfortrine(Synonyms: 雷公藤春碱)

Wilfortrine Chemical Structure

CAS No. : 37239-48-8

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生物活性

Wilfortrine is a bioactive sesquiterpene alkaloid. Wilfortrine exhibits immunosuppresive effects. Wilfortrine also can inhibit leukaemia cell growth in mice and shows anti-HIV activity[1].

分子量

873.81

Formula

C41H47NO20
CAS 号

37239-48-8
中文名称

雷公藤春碱
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Ouyang XK, et, al. Simultaneous determination of four sesquiterpene alkaloids in Tripterygium wilfordii Hook. F. extracts by high-performance liquid chromatography. Phytochem Anal. Jul-Aug 2007;18(4):320-5.

Wilfordine(Synonyms: 雷公藤碱；雷公藤定碱)

发表于由

天然产物 糖类和糖苷 Saccharides and Glycosides

Wilfordine;(Synonyms: 雷公藤碱；雷公藤定碱)

Wilfordine 是一种天然的生物碱，可以从 Tripterygium wilfordii 的根提取得到。

Wilfordine(Synonyms: 雷公藤碱；雷公藤定碱)

Wilfordine Chemical Structure

CAS No. : 37239-51-3

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生物活性

Wilfordine is an alkaloid that isolated from the roots of Tripterygium wilfordii[1].

分子量

883.84

Formula

C43H49NO19
CAS 号

37239-51-3
中文名称

雷公藤碱；雷公藤定碱
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Jianqun Liu, et al. Three new abietane-type diterpene glycosides from the roots of Tripterygium wilfordii. Fitoterapia. 2017 Jul;120:126-130.

Triptolide(Synonyms: 雷公藤甲素; PG490)

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Triptolide (Synonyms: 雷公藤甲素; PG490) 纯度: 99.78%

Triptolide是从雷公藤根中提取的二萜类三环氧化物，具有免疫抑制，抗炎，抗增殖和抗肿瘤作用。 雷公藤内酯是 NF-κB 活化的抑制剂。

Triptolide(Synonyms: 雷公藤甲素; PG490)

Triptolide Chemical Structure

CAS No. : 38748-32-2

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10 mM * 1 mL in DMSO ￥1150 In-stock
1 mg ￥520 In-stock
2 mg ￥910 In-stock
5 mg ￥1450 In-stock
10 mg ￥2250 In-stock
25 mg ￥4500 In-stock
100 mg ￥14500 In-stock
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生物活性

Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor[1][2][3][4][5][6].

IC50 & Target[1][2]

HSP90

 

MDM-2/p53

47-73 nM (IC50)

体外研究
(In Vitro)

Triptolide induces apoptosis in cultured and primary Chronic Lymphocytic Leukemia (CLL) B-cells. Treatment of CD19+ B cells with Triptolide, induces a dose-dependent increase in apoptosis in cultured and primary CLL cells. Triptolide is selectively toxic to both high risk (n=5) and low risk CLL (n=12) B cells (10 to 50 nM range) while largely sparing normal B-cells (n=5). Consistent with the inhibition of heat-shock induced HSP transcription, treatment with Triptolide attenuates heat-shock induced expression of HSPs[1]. Triptolide is a natural product derived from the Chinese plant Tripterygium wilfordii, is reported to exhibit antitumor effects in a broad range of cancers. Triptolide inhibits MDM2 expression in a dose-dependent manner, even at low concentrations spanning 20-100 nM in acute lymphoblastic leukemia (ALL) cells. Triptolide exhibits strongly cytotoxic activity in all 8 cell lines having native MDM2 overexpression, with IC50 values range from 47 to 73 nM. Triptolide exhibits much less cytotoxic effect on EU-4 cells that express very low level of MDM2, while it effectively kill these cells when MDM2 is stably transfected (IC50 values: 725 nM vs. 88 nM)[2]. Differentiated PC12 cells are incubated with different concentrations of Triptolide (0.01, 0.1, and 1 nM) in the presence of 10 μM Aβ25-35 for 24 hours and MTT assay is used to detect the effect of Triptolide. The results show that Aβ25-35 can decrease the cell viability and when treated with Triptolide the viability of differentiated PC12 cells is significantly increased. The results indicate that Triptolide can alleviate cellular damage caused by Aβ25-35, which means that Triptolide has a neuroprotective effect[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)

The Triptolide (TP) plasma concentrations are declined rapidly in mice after receive an intravenous dose. After 2h of injection, the Triptolide concentrations are dropped below the lower limit of quantification for all three groups. A comparison of the parameters is made between the control and the treated groups to assess the effect of P-gp inhibition on the Triptolide exposure and elimination. Treatment with the mdr1a-siRNA can significantly enhance the Triptolide plasma exposure, with the Cmax increases from 413±74 to 510±94 ng/mL (P<0.05) and the AUC from 103.5±9.6 to 154.3±30.2 ng•h/mL (P<0.05). In the concomitant group with Tariquidar, the significantly increased AUC is also noted, from 103.5±9.6 of the control to 145.9±24.6 ng•h/mL of the Triptolide+Tariquidar group (P<0.05). Accordingly, the total body clearance of Triptolide in mice is remarkably decreased, from 9564±1024.2 mL/min/kg of the control to 6576.4±1438.5 (P<0.05) and 5755.4±1200.1 mL/min/kg (P<0.05) for Triptolide+Tariquidar and Triptolide+mdr1a-siRNA groups, respectively[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

360.40

Formula

C20H24O6
CAS 号

38748-32-2
中文名称

雷公藤甲素；雷藤素甲；雷公藤内酯醇；雷公藤多甙
运输条件

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

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : ≥ 33 mg/mL (91.56 mM)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

* “≥” 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 2.7747 mL 13.8735 mL 27.7469 mL
5 mM 0.5549 mL 2.7747 mL 5.5494 mL
10 mM 0.2775 mL 1.3873 mL 2.7747 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 (stored under nitrogen)。-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: ≥ 1.17 mg/mL (3.25 mM); Clear solution

    此方案可获得 ≥ 1.17 mg/mL (3.25 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 11.7 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: ≥ 1.17 mg/mL (3.25 mM); Clear solution

    此方案可获得 ≥ 1.17 mg/mL (3.25 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 11.7 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: ≥ 1.17 mg/mL (3.25 mM); Clear solution

    此方案可获得 ≥ 1.17 mg/mL (3.25 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 11.7 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]. Ganguly S, et al. Targeting HSF1 disrupts HSP90 chaperone function in chronic lymphocytic leukemia. Oncotarget. 2015 Oct 13;6(31):31767-79.

    [2]. Huang M, et al. Triptolide inhibits MDM2 and induces apoptosis in acute lymphoblastic leukemia cells through a p53-independent pathway. Mol Cancer Ther. 2013 Feb;12(2):184-94.

    [3]. Xu P, et al. Triptolide Inhibited Cytotoxicity of Differentiated PC12 Cells Induced by Amyloid-Beta25-35 via the Autophagy Pathway. PLoS One. 2015 Nov 10;10(11):e0142719.

    [4]. Kong LL, et al. Inhibition of P-glycoprotein Gene Expression and Function Enhances Triptolide-induced Hepatotoxicity in Mice. Sci Rep. 2015 Jul 2;5:11747.

    [5]. Zhang W, et al. Triptolide Combined with Radiotherapy for the Treatment of Nasopharyngeal Carcinoma via NF-κB-Related Mechanism. Int J Mol Sci. 2016 Dec 19;17(12). pii: E2139.

    [6]. Cai J, et al. Natural product triptolide induces GSDME-mediated pyroptosis in head and neck cancer through suppressing mitochondrial hexokinase-ΙΙ. J Exp Clin Cancer Res. 2021;40(1):190. Published 2021 Jun 9.
Cell Assay
[3]

The viability of differentiated PC12 cells treated with different concentrations of Triptolide. After differentiated PC12 cells are cultured on 96-well plates with RPMI 1640 medium for stabilization, differentiated PC12 cells are incubated with different concentrations of Triptolide (0.01, 0.1, and 1 nM) for 24 hours. The concentrations in this study are chosen. Then cell viability is determined by the MTT assay. Each condition and experiment is repeated three times[3].

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

Mice[4]
Male BALB/C mice (weight, 18-22 g) are used. For Triptolide (TP) plasma kinetic study and toxicological evaluation, mice are divided into four groups (n=5 each) to collect blood and tissue samples: (1) normal+saline group; (2) 1.0 mg/kg Triptolide+15 nmol negative control (NC) siRNA-siRNA group; (3) 1.0 mg/kg Triptolide+15 nmol mdr1a-siRNA group; (4) 1.0 mg/kg Triptolide+10 mg/kg Tariquidar group. In order to avoid the complication caused by drug absorption or possible intestinal first-pass effect, Triptolide and the inhibitor are intravenously administrated to mice. The siRNA group is intravenously injected with NC-siRNA or mdr1a-siRNA 2 days before Triptolide dose. For Triptolide+Tariquidar group, the mice are received an intravenous Tariquidar dose 20 min prior to the Triptolide injection. Blood samples are collected at 2, 5, 10, 15, 30, 60 and 120 min after Triptolide dosing. To assess the liver exposure of Triptolide, liver tissue samples are collected from another set of mice at 5, 30, 60 and 120 min after dosing. Three Triptolide groups are design for this experiment, including Triptolide+NC-siRNA group, Triptolide+mdr1a-siRNA group and Triptolide+Tariquidar group. The liver tissue samples are weighed and then homogenized in 10 volume (w:v) of ice-cold saline. The concentrations of Triptolide in plasma and liver tissue are measured by a validated LC-MS/MS method.

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

  • [1]. Ganguly S, et al. Targeting HSF1 disrupts HSP90 chaperone function in chronic lymphocytic leukemia. Oncotarget. 2015 Oct 13;6(31):31767-79.

    [2]. Huang M, et al. Triptolide inhibits MDM2 and induces apoptosis in acute lymphoblastic leukemia cells through a p53-independent pathway. Mol Cancer Ther. 2013 Feb;12(2):184-94.

    [3]. Xu P, et al. Triptolide Inhibited Cytotoxicity of Differentiated PC12 Cells Induced by Amyloid-Beta25-35 via the Autophagy Pathway. PLoS One. 2015 Nov 10;10(11):e0142719.

    [4]. Kong LL, et al. Inhibition of P-glycoprotein Gene Expression and Function Enhances Triptolide-induced Hepatotoxicity in Mice. Sci Rep. 2015 Jul 2;5:11747.

    [5]. Zhang W, et al. Triptolide Combined with Radiotherapy for the Treatment of Nasopharyngeal Carcinoma via NF-κB-Related Mechanism. Int J Mol Sci. 2016 Dec 19;17(12). pii: E2139.

    [6]. Cai J, et al. Natural product triptolide induces GSDME-mediated pyroptosis in head and neck cancer through suppressing mitochondrial hexokinase-ΙΙ. J Exp Clin Cancer Res. 2021;40(1):190. Published 2021 Jun 9.

Tripterin(Synonyms: 雷公藤红素; Celastrol)

发表于由

上海金畔生物科技有限公司提供天然产物萜类及其苷类Terpenoids and Glycosides。

Tripterin (Synonyms: 雷公藤红素; Celastrol) 纯度: 99.65%

Tripterin (Celastrol) 是一种蛋白酶体抑制剂，有效且优先抑制20S 蛋白酶体的胰凝乳蛋白酶样活性，IC50 为2.5 μM。

Tripterin(Synonyms: 雷公藤红素; Celastrol)

Tripterin Chemical Structure

CAS No. : 34157-83-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥921 In-stock
10 mg ￥837 In-stock
50 mg ￥2325 In-stock
100 mg ￥3255 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.

IC50 & Target

IC50: 2.5 μM (20S proteasome)[1]
体外研究
(In Vitro)

Tripterin (Celastrol) significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner; at 2.5 μM it reaches ~55% inhibition, comparable to its potency to a purified 20S proteasome (IC50=2.5 μM). Furthermore, increased levels of IκB-α, Bax, and p27 are observed, three well known target proteins of the proteasome in PC-3 cells treated with Celastrol[1].

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)

Treatment of PC-3 tumor-bearing nude mice with Tripterin (Celastrol) (1-3 mg/kg/d, i.p., 1-31 days) results in significant inhibition (65-93%) of the tumor growth[1]. Following treatment with 3 and 6 mg/kg Tripterin (Celastrol), the levels of malondialdehyde (MDA) are significantly decreased by 35.2 and 36.7% (P<0.05), respectively. Treatment with 3 and 6 mg/kg Tripterin (Celastrol) markedly restores the GSH level (P<0.05) to almost normal levels[2].

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

450.61

Formula

C29H38O4
CAS 号

34157-83-0
中文名称

雷公藤红素；南蛇藤素；南蛇藤醇；苦瓜甙；苦瓜苷；苦瓜素；苦瓜皂甙
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 : 33.33 mg/mL (73.97 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2192 mL 11.0961 mL 22.1921 mL
5 mM 0.4438 mL 2.2192 mL 4.4384 mL
10 mM 0.2219 mL 1.1096 mL 2.2192 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 (5.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.55 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

*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 H, et al. Celastrol, a triterpene extracted from the Chinese “Thunder of God Vine,” is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Cancer Res. 2006 May 1;66(9):4758-65

    [2]. Guan Y, et al. Celastrol attenuates oxidative stress in the skeletal muscle of diabetic rats by regulating the AMPK-PGC1α-SIRT3 signaling pathway. Int J Mol Med. 2016 May;37(5):1229-38.
Kinase Assay
[1]

A purified rabbit 20S proteasome (0.1 μg) is incubated with 40 μM of various fluorogenic peptide substrates in 100 μL assay buffer (20 mM Tris-HCl ,pH 7.5), in the presence of Celastrol or Oridonin at different concentrations or in the solvent DMSO for 2 hours at 37°C, followed by measurement of inhibition of each proteasomal activity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Prostate cancer cells (5,000-8,000) are plated in each well of a 96-well plate and then treated with either DMSO, Tripterin (Celastrol), or Oridonin at different concentrations for 12 to 16 hours, followed by an additional 2-hour incubation with Z-Gly-Gly-Leu-AMC (at 40 μM). After that, the proteasome activity is measured using the whole plate[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][2]

Mice[1]
Male nude immunodeficient mice NCRNU-M, aged 5 weeks, are used. On day 0, human prostate cancer PC-3 or C4-2B cells (5-10×106) suspended in 0.1 mL of serum-free RPMI 1640 are inoculated s.c. in the right flank of each mouse (four mice per group). For the first experiment using PC-3 cells, on day 14 after inoculation, the animals started daily i.p. injection with either 50 to 100 μL of a vehicle [10% DMSO, 70% Cremophor/ethanol (3:1), and 20% PBS], and 1.0 or 3.0 mg/kg of Tripterin (Celastrol) . Tumor sizes are measured daily using calipers and their volumes are calculated using a standard formula: width2×length/2. Body weight is measured weekly. To study whether the proteasome is inhibited in an early phase of the experiment, after 3 days of treatment, one control and one 3.0 mg/kg Tripterin (Celastrol) -treated mouse is sacrificed. The rest are sacrificed after 16 days of treatment when control tumors reach 1,400 mm3. For the second PC-3 tumor experiment, 12 days after inoculation, mice are randomly divided into three groups and treated with either control, Tripterin (Celastrol) , or Oridonin at 1.5 mg/kg daily for the duration of the study (31 days). In another experiment, to study the effects of Tripterin (Celastrol) on AR expression, nude mice bearing C4-2B tumors receive daily i.p. injection of the vehicle or 3.0 mg/kg Tripterin (Celastrol) .
Rats[2]
Male Sprague-Dawley (SD) rats (n=90, 6 weeks old), weighing 161±9 g, are randomly divided into the control (NC) and the high energy diet (HED) groups. In the control group, the animals receive a standard chow diet, while the rats in the HED group are fed with an additional high energy emulsion. After 8 weeks on their respective diets, Streptozotocin (STZ; 45 mg/kg) dissolved in 0.1 mol/l citrate buffer (pH 4.5) is injected into the caudal vein of the rats in the HED group to establish a model of T2DM, while the rats in the control group are injected with sodium citrate buffer. The rats with blood glucose levels ≥16.7 mM at 7 days after the STZ injection are selected as the model of diabetes. On average, 80% of the rats injected with STZ met these criteria. At 1 week following the injection of STZ, the rats with successfully-induced diabetes are randomly divided into the diabetes model (DM) group, the Tripterin (Celastrol) low-dose group (1 mg/kg/day), the Tripterin (Celastrol) middle-dose group (3 mg/kg/day) and the Tripterin (Celastrol) high-dose group (6 mg/kg/day) (n=15 rats per group). The rats in the treatment groups are administered Tripterin (Celastrol) by gavage, whereas the rats in the NC and DM groups are administered an equal amount of distilled water (2 mL). Following 8 weeks of the respective treatments, rats are anesthetized with an intraperitoneal injection of sodium pentobarbital (30 mg/kg body weight) and tissue samples are collected for analysis. The paravertebral muscle is excised from the rat bodies, and is cut perpendicularly along the longitudinal axis and fixed in phosphate-buffered 20% formaldehyde. Histological paraffin-embedded sections (5 µm) are then prepared for H&E staining. The sections of paravertebral muscle are snap-frozen in liquid nitrogen and stored at −80°C until further analysis.

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 H, et al. Celastrol, a triterpene extracted from the Chinese “Thunder of God Vine,” is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Cancer Res. 2006 May 1;66(9):4758-65

    [2]. Guan Y, et al. Celastrol attenuates oxidative stress in the skeletal muscle of diabetic rats by regulating the AMPK-PGC1α-SIRT3 signaling pathway. Int J Mol Med. 2016 May;37(5):1229-38.

Triptonide(Synonyms: 雷公藤内酯酮; NSC 165677; PG 492)

发表于由

上海金畔生物科技有限公司提供天然产物萜类及其苷类Terpenoids and Glycosides。

Triptonide (Synonyms: 雷公藤内酯酮; NSC 165677; PG 492) 纯度: 99.73%

Triptonide (NSC 165677) 是从雷公藤中鉴定出的一种天然产物。Triptonide 是一种 Wnt 信号抑制剂，其 IC50 约为 0.3 nM。Triptonide 具有免疫抑制、抗炎、避育、神经保护和抗淋巴瘤作用。

Triptonide(Synonyms: 雷公藤内酯酮; NSC 165677; PG 492)

Triptonide Chemical Structure

CAS No. : 38647-11-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2251 In-stock
10 mg ￥2046 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

Triptonide (NSC 165677) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC50 of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects[1][2].

IC50 & Target

IC50: 0.3 nM (Wnt)[1]
体外研究
(In Vitro)

Triptonide blocks Wnt/β-catenin signaling via C-terminal transactivation domain of β-catenin, and promots apoptosis in Wnt-dependent cancer cells[1].
Triptonide potently inhibits the proliferation of human B-lymphoma Raji and T-lymphoma Jurkat cells with IC50 of 5.7 nM and 4.8 nM, respectively[2].
Triptonide (2.5-10 nM; 6 days) significantly suppresses B-lymphoma cell colony-forming capability[2].
Triptonide (20 nM; 3 days) promotes apoptosis through activation of PARP and caspase 3, but reduction of BCL2 protein levels in the lymphoma cells[2].
Triptonide (5-10 nM; 72 hours) markedly reduces both total and phosphorylated Lyn proteins, and diminishes Lyn downstream ERK and ATK signal pathways[2].

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

Cell Proliferation Assay[2]

Cell Line: B-lymphoma Raji cells, T-lymphoma Jurkat cells
Concentration: 0-80 nM
Incubation Time: 3 days, 6 days
Result: Inhibited lymphoma cell tumorigenic capability in a dose-dependent manner.

Apoptosis Analysis[2]

Cell Line: Raji cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 3 days
Result: Did not significantly induce apoptosis at the effective tumor growth-inhibitory (2.5-10 nM); moderately induced lymphoma cell apoptosis (20 nM).

Western Blot Analysis[2]

Cell Line: Raji cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 3 days
Result: Did not vigorously activated pro-apoptotic proteins PARP and caspase 3 in lymphoma cells (5-10 nM); significantly activated PARP and caspase 3 (20 nM); significantly reduced anti-apoptotic BCL2 levels.

RT-PCR[2]

Cell Line: Raji cells
Concentration: 5 nM, 10 nM
Incubation Time: 72 hours
Result: Significantly diminished Lyn mRNA levels in the lymphoma cells.

体内研究
(In Vivo)

Triptonide (5 mg/kg; i.p.; daily; for 34 days) exerts a strong anti-lymphoma effect in mice[2].

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

Animal Model: Eight-week-old female NOD/SCID mice (18-22 g), with 3 x 107 Raji cells xenograft[2]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, daily, for 34 days
Result: Potently inhibited lymphoma cell growth and tumorigenic capability.

分子量

358.39

Formula

C20H22O6
CAS 号

38647-11-9
中文名称

雷公藤内酯酮；雷藤酮；雷公藤羰内酯
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 : 100 mg/mL (279.03 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7903 mL 13.9513 mL 27.9026 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL
10 mM 0.2790 mL 1.3951 mL 2.7903 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    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.98 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]. Jessica Chinison, et al. Triptonide Effectively Inhibits Wnt/β-Catenin Signaling via C-terminal Transactivation Domain of β-catenin. Sci Rep. 2016; 6: 32779.

    [2]. Ping Yang, et al. Triptonide acts as a novel potent anti-lymphoma agent with low toxicity mainly through inhibition of proto-oncogene Lyn transcription and suppression of Lyn signal pathway. Toxicol LettPing Yang. 2017 Aug 15;278:9-17.

Wilforlide A(Synonyms: 雷公藤内酯甲; Regelide; Abruslactone A)

发表于由

上海金畔生物科技有限公司提供天然产物萜类及其苷类Terpenoids and Glycosides。

Wilforlide A (Synonyms: 雷公藤内酯甲; Regelide; Abruslactone A) 纯度: ≥98.0%

Wilforlide A 是从雷公藤中分离得到的一种生物活性三萜，具有抗炎和免疫抑制作用。

Wilforlide A(Synonyms: 雷公藤内酯甲; Regelide; Abruslactone A)

Wilforlide A Chemical Structure

CAS No. : 84104-71-2

规格 价格 是否有货 数量
5 mg ￥950 In-stock
10 mg ￥1350 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

Wilforlide A is a bioactive triterpene isolated from Tripterygium wilfordii Hook f. Wilforlide A has anti-inflammatory and immune suppressive effects[1].

体内研究
(In Vivo)

Wilforlide A (60-300 μg/kg) markedly inhibits mice auricular swelling induced by dimethylbenzene in ICR mice. Wilforlide A exhibits inhibition rates with 50.9% and 12.29% for high dose and low dose Wilforlide A, resepectively[1]. Wilforlide A (30-150 μg/kg) markedly inhibits rat granulation induced by tampon[1].

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

454.68

Formula

C30H46O3
CAS 号

84104-71-2
中文名称

雷公藤内酯甲；雷公藤内酯 A
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 : 1 mg/mL (2.20 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1993 mL 10.9967 mL 21.9935 mL
5 mM — — —
10 mM — — —

*

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]. Mei Xue, et al. Comparative study on the anti-inflammatory and immune suppressive effect of Wilforlide A. Fitoterapia

Wilforgine(Synonyms: 雷公藤精碱)

发表于由

上海金畔生物科技有限公司提供天然产物萜类及其苷类Terpenoids and Glycosides。

Wilforgine (Synonyms: 雷公藤精碱) 纯度: 99.67%

Wilforgine 是 Tripterygium wilfordii Hook. F 中的生物活性倍半萜烯生物碱。Wilforgine 能诱导分离出丝状体幼虫肌肉的微结构和超微结构变化，其作用部位被认为是肌肉系统中的钙受体或通道。

Wilforgine(Synonyms: 雷公藤精碱)

Wilforgine Chemical Structure

CAS No. : 37239-47-7

规格 价格 是否有货 数量
5 mg ￥2690 In-stock
10 mg ￥4570 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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•相关化合物库:

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  • Traditional Chinese Medicine Monomer Library

生物活性

Wilforgine is a bioactive sesquiterpene alkaloid in Tripterygium wilfordii Hook. F. Wilforgine can induce microstructural and ultrastructural changes in the muscles of Mythimna separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system[1][2].

分子量

857.81

Formula

C41H47NO19
CAS 号

37239-47-7
中文名称

雷公藤精碱
运输条件

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

4°C, protect from light

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

DMSO : 100 mg/mL (116.58 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 1.1658 mL 5.8288 mL 11.6576 mL
5 mM 0.2332 mL 1.1658 mL 2.3315 mL
10 mM 0.1166 mL 0.5829 mL 1.1658 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 (protect from 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: ≥ 2.5 mg/mL (2.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.91 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% corn oil

    Solubility: ≥ 2.5 mg/mL (2.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.91 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]. Ouyang XK, et al. Simultaneous determination of four sesquiterpene alkaloids in Tripterygium wilfordii Hook. F. extracts by high-performance liquid chromatography. Phytochem Anal. 2007 Jul-Aug;18(4):320-5.

    [2]. Ma S, et al. Comparative studies on muscle microstructure and ultrastructure of Mythimna separata Walker treated with wilforgine and chlorantraniliprole. Ecotoxicol Environ Saf. 2018 Jan;147:1023-1034.

    [3]. Gao X, et al. Wilforine, the Q-marker and PK-maker of Tripterygium glycosides tablet: Based on preparation quantitative analysis and PK-PD study. Phytomedicine. 2019 Feb 15;54:357-364.