GsMTx4 TFA

GsMTx4 TFA; 纯度: 98.29%

GsMTx4 TFA 是一种蜘蛛毒液肽,选择性地抑制属于 Piezo 和 TRP 通道家族的阳离子可渗透的机械敏感性通道 (MSCs)。GsMTx4 TFA 是一种重要的药理学工具,用于鉴定兴奋性 MSCs 在正常生理学和病理学中的作用。GsMTx4 TFA 显着减弱膀胱机能亢进。

GsMTx4 TFAamp;;

GsMTx4 TFA Chemical Structure

规格 价格 是否有货 数量
500 μg ¥2700 In-stock
1 mg ¥5000 In-stock
5 mg ¥18000 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

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GsMTx4 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

GsMTx4 TFA is a spider venom peptide that selectively inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology[1]. GsMTx4 TFA significantly attenuates bladder hyperactivity[2].

IC50 Target

MSCs[1]

分子量

4215.91

Formula

C187H280N49F3O47S6

Sequence Shortening

GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro:;

DMSO : 10 mg/mL (2.37 mM; Need ultrasonic)

H2O : < 0.1 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 0.2372 mL 1.1860 mL 2.3720 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 (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。

参考文献
  • [1]. Gnanasambandam R, et al. GsMTx4: Mechanism of Inhibiting Mechanosensitive Ion Channels. Biophys J. 2017 Jan 10;112(1):31-45.

    [2]. Liu Q, et al. Increased Piezo1 channel activity in interstitial Cajal-like cells induces bladder hyperactivity by functionally interacting with NCX1 in rats with cyclophosphamide-induced cystitis. Exp Mol Med. 2018 May 7;50(5):60.

GRGDSP TFA

GRGDSP TFA; 纯度: ge;98.0%

GRGDSP (TFA) 是一种整联蛋白 (integrin) 抑制剂。

GRGDSP TFAamp;;

GRGDSP TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ¥880 In-stock
5 mg ¥1650 In-stock
10 mg ¥2850 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

GRGDSP TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptidomimetic Library
  • Peptide Library

生物活性

GRGDSP (TFA) is an integrin inhibitor.

IC50 Target

Integrin[1].

体外研究
(In Vitro)

It is demonstrated that transarterial infusion of GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro integrin-inhibitor which includes RGD-peptide). As a synthetic linear RGD peptide, GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro) can inhibit the adherence of tumor cells to endothelial cells of blood vessels and limit its metastasis[1]. GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro) is used as a soluble integrin-blocking RGD-based peptide. GRGDSP is used widely together with other RGD peptides in integrin research. GRGDSP can be used to modify the surface of cardiovascular implants such as vascular grafts to promote endothelialization[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

701.61

Formula

C24H38F3N9O12

Sequence

Gly-Arg-Gly-Asp-Ser-Pro

Sequence Shortening

GRGDSP

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

H2O : 125 mg/mL (178.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4253 mL 7.1265 mL 14.2529 mL
5 mM 0.2851 mL 1.4253 mL 2.8506 mL
10 mM 0.1425 mL 0.7126 mL 1.4253 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)。-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]. Qian J, et al. Transarterial administration of integrin inhibitor loaded nanoparticles combined with transarterial chemoembolization for treating hepatocellular carcinoma in a rat model. World J Gastroenterol. 2016 Jun 7;22(21):5042-9.

    [2]. Patel S, et al. Regulation of endothelial cell function by GRGDSP peptide grafted on interpenetrating polymers. J Biomed Mater Res A. 2007 Nov;83(2):423-33.

PKA Inhibitor Fragment (6-22) amide TFA(Synonyms: PKI-(6-22)-amide TFA)

PKA Inhibitor Fragment (6-22) amide TFA;(Synonyms: PKI-(6-22)-amide TFA) 纯度: 96.71%

PKA Inhibitor Fragment (6-22) amide TFA 是 cAMP 依赖性蛋白激酶 A (PKA) 的抑制剂,Ki 值为 2.8 nM。PKA Inhibitor Fragment (6-22) amide TFA 可显着逆转小鼠低水平的吗啡缓解疼痛的感受性。

PKA Inhibitor Fragment (6-22) amide TFAamp;;(Synonyms: PKI-(6-22)-amide TFA)

PKA Inhibitor Fragment (6-22) amide TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ¥2100 In-stock
10 mg ¥3500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

PKA Inhibitor Fragment (6-22) amide TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice[1][2].

IC50 Target

PKA

2.8 nM (Ki)

分子量

1982.08

Formula

C82H131F3N28O26

Sequence Shortening

TYADFIASGRTGRRNAI-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

H2O : 50 mg/mL (25.23 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5045 mL 2.5226 mL 5.0452 mL
5 mM 0.1009 mL 0.5045 mL 1.0090 mL
10 mM 0.0505 mL 0.2523 mL 0.5045 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)。-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]. Katz BM, et, al. Synthesis, characterization and inhibitory activities of (4-N3[3,5-3H]Phe10)PKI(6-22)amide and its precursors: photoaffinity labeling peptides for the active site of cyclic AMP-dependent protein kinase. Int J Pept Protein Res. 1989 Jun;33(6):439-45.

    [2]. Dalton GD, et, al. Alterations in brain Protein Kinase A activity and reversal of morphine tolerance by two fragments of native Protein Kinase A inhibitor peptide (PKI). Neuropharmacology. 2005 Apr; 48(5): 648-57.

Colivelin TFA

Colivelin TFA; 纯度: 99.22%

Colivelin TFA 是一种具有大脑通透性的神经保护肽 (neuroprotective peptide),是 STAT3 的有效激活剂。Coliveli 通过激活 STAT3 在体外抑制神经元死亡。Colivelin TFA 对神经毒性、Aβ 沉积,神经元细胞凋亡,在神经退行性疾病显示出长期有利的影响。Colivelin TFA 可用于阿尔茨海默病和缺血性脑损伤的相关研究。

Colivelin TFAamp;;

Colivelin TFA Chemical Structure

规格 价格 是否有货 数量
500 μg ¥2280 In-stock
1 mg ¥3480 In-stock
5 mg ; 询价 ;
10 mg ; 询价 ;

* Please select Quantity before adding items.

Colivelin TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro[1]. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease[2]. Colivelin TFA has the potential for the treatment of alzheimer’s disease and ischemic brain injury[1].

IC50 Target[1]

STAT3

;

Amyloid-β

;

体外研究
(In Vitro)

Colivelin completely suppresses death induced by overexpressed FAD-causative genes and Aβ1-43 at a concentration of 100 fm, and keep its neuroprotective action at or above the levels of 1 nm[1].
Colivelin-induced neuroprotection occurs via two neuroprotective pathways: one mediated by Ca2+/calmodulin-dependent protein kinase IV, triggered by ADNF, and one mediated by signal transducer and activator of transcription 3, triggered by HN[1].
Colivelin reverses caspase3, Bax and Bcl-2 expressions in HT22 cells medaited by rmMFG-E8 in the co-cultured cells under OGD condition[4].
Colivelin (50 µg/mL, 4 hours) significantly increases the p-STAT3 protein levels in BV-2 cells[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[4]

Cell Line: BV-2 cells.
Concentration: 50 µg/mL.
Incubation Time: 4 hours.
Result: Increased p-STAT3 levels.

Cell Viability Assay[5]

Cell Line: KYSE70 and TE8 cells.
Concentration: 0.5 μM.
Incubation Time: 1 hour (followed by CYT-Rx20 treatment)
Result: Significantly suppressed the viability in KYSE70 and TE8 cells.

体内研究
(In Vivo)

Colivelin(intracerebroventricular administration; 10 pmol/3 μl; 3 weeks) suppresses impairment in spatial working memory induced by repetitive intracerebroventricular injection of Aβ25-35 or Aβ1-42, in addition, it antagonizes neuronal loss in the CA1 region of hippocampus induced by hippocampal injection of Aβ1-42[1].
Colivelin (intraperitoneal administration; 1.4, 7, or 35 nM/0.21mL; on the Y-maze testday) suppresses memory impairment caused by 3-quinuclidinyl benzilateand restricts functional memory deficit[1].
Colivelin (intraperitoneal injection; 1 mg/kg; 14 days) results in improved motor and cognitive function with time by performance of mNSS, rotarod, and corner turning test.It also reduces lesion volume and improves neurological deficits after MCAO[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 mice[1]
Dosage: 10 pmol/3 μl
Administration: Intracerebroventricular administration
Result: Completely suppressed Aβ 25-35-mediated impairment in spatial working memory and increased the number of immunoreactive neurons.
Animal Model: C57 mice[1]
Dosage: 1.4, 7, or 35 nM/0.21mL
Administration: Intraperitoneal administration
Result: Protected against cholinotoxin-induced amnesia in mice.
Animal Model: Male C57BL/6 mice[3]
Dosage: 1 mg/kg
Administration: Intraperitoneal administration
Result: Protected against ischemic brain injury, and improves neurological outcomes.

分子量

2759.12

Formula

C119H206N32O35.C2HF3O2

Sequence Shortening

SALLRSIPAPAGASRLLLLTGEIDLP

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

H2O : 50 mg/mL (18.12 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.3624 mL 1.8122 mL 3.6243 mL
5 mM 0.0725 mL 0.3624 mL 0.7249 mL
10 mM 0.0362 mL 0.1812 mL 0.3624 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)。-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:;Water with 5% sefsol and 20% isopropanol

    Solubility: 6.25 mg/mL (2.27 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Chiba T, et al. Development of a femtomolar-acting humanin derivative named colivelin by attaching activity-dependent neurotrophic factor to its N terminus: characterization of colivelin-mediated neuroprotection against Alzheimer’s disease-relevant insults in vitro and in vivo. J Neurosci. 2005 Nov 2;25(44):10252-61.

    [2]. Zhao H, et al. Colivelin Rescues Ischemic Neuron and Axons Involving JAK/STAT3 Signaling Pathway.Neuroscience. 2019 Sep 15;416:198-206.

    [3]. Pan Z, et al. Upregulation of HSP72 attenuates tendon adhesion by regulating fibroblast proliferation and collagen production via blockade of the STAT3 signaling pathway.Cell Signal. 2020 Mar 18:109606.

    [4]. Fang YY, et al. MFG-E8 alleviates oxygen-glucose deprivation-induced neuronal cell apoptosis by STAT3 regulating the selective polarization of microglia. Int J Neurosci. 2020 Mar 12:1-10.

    [5]. Chiu WC, et al. The Synthetic β-Nitrostyrene Derivative CYT-Rx20 Inhibits Esophageal Tumor Growth and Metastasis via PI3K/AKT and STAT3 Pathways. PLoS One. 2016 Nov 22;11(11):e0166453.

FSL-1 TFA

FSL-1 TFA; 纯度: 99.58%

FSL-1 TFA 是细菌衍生的一种 Toll 样受体 2/6 (TLR2/6) 激动剂,可增强对 HSV-2 感染的抵抗力。FSL-1 TFA 通过 TLR2NF-κB/AP-1 信号通路诱导 MMP-9 产生。

FSL-1 TFAamp;;

FSL-1 TFA Chemical Structure

规格 价格 是否有货 数量
100 μg ¥1600 In-stock

* Please select Quantity before adding items.

生物活性

FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection[1]. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells[2].

IC50 Target[1][2]

TLR2

;

TLR6

;

MMP-9

;

体外研究
(In Vitro)

FSL-1 significantly reduces HSV-2 replication in human vaginal epithelial cells (EC)[1].
FSL-1 induces significant resistance to experimental genital HSV-2 infection through elaboration of a specific cytokine response profile[1].
FSL-1 (50 ng/mL, 24 hours) induces MMP-9 expression at both mRNA and protein levels in human monocytic THP-1 cells[2].
FSL-1 activates the MAP kinase/NF-κB signaling pathway[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: V11I, V12I or V19I immortalized human vaginal EC
Concentration: 6 μg or 0.1 μg
Incubation Time: Added at 24, 6 or just prior to HSV-2 inoculation (104pfu/well)
Result: The 6 μg does produced significant reductions when delivered at 24 or 6 h prior to HSV-2 inoculation. The 0.1 μg dose produced reduced HSV-2 replication at 24 or 6 h prior to viral challenge.

体内研究
(In Vivo)

FSL-1 application significantly protectes against genital HSV-2 challenge in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Swiss-Webster mice (weighing 20-25 g)[1]
Dosage: 2 or 6 μg
Administration: Delivered vaginally using a positive displacement pipet, prior to or following viral challenge as specified for each experiment.
Result: The 2 μg does delivered 6 h prior to HSV-2 challenge increased the ID50 (260 pfu) and LD50 (660 pfu) by 10-fold compared to DPBS vehicle control.
The single 6 μg dose produced significantly improved outcomes compared to DPBS vehicle application.

分子量

1780.18

Formula

C82H141F3N14O20S

Sequence Shortening

S-(2, 3-Bispalmitoyloxypropyl)-CGDPKHPKSF

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)

Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
  • [1]. William A Rose 2nd, et al. FSL-1, a bacterial-derived toll-like receptor 2/6 agonist, enhances resistance to experimental HSV-2 infection. Virol J. 2009 Nov 10;6:195.

    [2]. Cathryn J Kurkjian,et al. The Toll-Like Receptor 2/6 Agonist, FSL-1 Lipopeptide, Therapeutically Mitigates Acute Radiation Syndrome. Sci Rep. 2017 Dec 11;7(1):17355.

ATI-2341 TFA

ATI-2341 TFA; 纯度: 98.11%

ATI-2341 是一种有效的 C-X-C 趋化因子受体 4 型 (CXCR4) 功能选择性变构激动剂,其作为偏向配体起作用,有利于 Gα1激活而不是 Gα13。ATI-2341 激活抑制性异源三聚体 G 蛋白 (Gi) 以促进 cAMP 产生的抑制并诱导钙动员。ATI-2341 是一种有效骨髓多形核中性粒细胞 (PMNs) 和造血干细胞和祖细胞 (HSPCs) 动员剂。

ATI-2341 TFAamp;;

ATI-2341 TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ¥1400 In-stock
5 mg ¥3900 In-stock
10 mg ¥6100 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

ATI-2341 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs)[1][2].

体外研究
(In Vitro)

CXCR4[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

2370.84

Formula

C106H179F3N26O27S2

Sequence Shortening

1-Oxohexadecyl-MGYQKKLRSMTDKYRL

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

DMSO : 100 mg/mL (42.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.4218 mL 2.1090 mL 4.2179 mL
5 mM 0.0844 mL 0.4218 mL 0.8436 mL
10 mM 0.0422 mL 0.2109 mL 0.4218 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)。-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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (1.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.05 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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (1.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.05 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 MCE 网站选购。
参考文献
  • [1]. Quoyer J, et al. Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein. Proc Natl Acad Sci U S A. 2013 Dec 24;110(52):E5088-97.

    [2]. Tchernychev B, et al. Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells. Proc Natl Acad Sci U S A. 2010 Dec 21;107(51):22255-9.

Dynorphin A (1-10) (TFA)

Dynorphin A (1-10) (TFA); 纯度: 99.43%

Dynorphin A (1-10) (TFA) 是一种内源性的阿片样神经肽,与 κ 阿片受体 (κ-opioid receptor) 结合。Dynorphin A (1-10) (TFA) 也阻断 NMDA 激活的电流,IC50 为 42.0 μM。

Dynorphin A (1-10) (TFA)amp;;

Dynorphin A (1-10) (TFA) Chemical Structure

规格 价格 是否有货 数量
1 mg ¥1100 In-stock
5 mg ¥3600 In-stock
10 mg ¥5600 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Dynorphin A (1-10) (TFA) 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.

IC50 Target

κ-opioid receptor[1]
IC50: 42.0 μM (NMDA receptor)[2]

体外研究
(In Vitro)

Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds in the transmembrane domain of the κ-receptor[1]. The non-opioid actions of various forms of Dynorphin A (DynA) are examined on N-methyl-D-aspartate (NMDA) receptor channels in isolated rat trigeminal neurons using the whole-cell patch recording technique. All the dynorphins tested blocked NMDA-activated currents. The blocking actions are voltage-independent. The IC50 is 42.0 μM for DynA(1-10). To determine if shorter dynorphins have the similar blocking property, we examined the action of DynA(1-10) at different membrane potentials. DynA(1-10) blocks INMDA to a similar extent as the membrane potentials changed from -80 to +60 mV. Thus, despite a 160-fold difference in the apparent affinities, DynA(1-32) and DynA(1-10) both exert voltage-independent actions on NMDA receptors[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1348.48

Formula

C59H92F3N19O14

Sequence

Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro

Sequence Shortening

YGGFLRRIRP

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

DMSO : 100 mg/mL (74.16 mM; Need ultrasonic)

H2O : 50 mg/mL (37.08 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7416 mL 3.7079 mL 7.4158 mL
5 mM 0.1483 mL 0.7416 mL 1.4832 mL
10 mM 0.0742 mL 0.3708 mL 0.7416 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)。-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 (1.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.85 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 (1.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.85 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 (1.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.85 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 MCE 网站选购。
参考文献
  • [1]. Paterlini G, et al. Molecular simulation of dynorphin A-(1-10) binding to extracellular loop 2 of the kappa-opioidreceptor. A model for receptor activation. J Med Chem. 1997 Sep 26;40(20):3254-62.

    [2]. Chen L, et al. Dynorphin block of N-methyl-D-aspartate channels increases with the peptide length. J Pharmacol Exp Ther. 1998 Mar;284(3):826-31.

DTP3 TFA

DTP3 TFA; 纯度: 98.75%

DTP3 TFA 是一种有效且选择性的 GADD45β/MKK7 抑制剂。DTP3 TFA 靶向 NF-κB 途径下游,具有抗癌活性。

DTP3 TFAamp;;

DTP3 TFA Chemical Structure

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ¥2251 In-stock
5 mg ¥1600 In-stock
10 mg ¥2800 In-stock
25 mg ¥4000 In-stock
50 mg ¥5500 In-stock
100 mg ¥8000 In-stock
200 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

DTP3 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • NF-kappa;B Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Anti-Obesity Compound Library
  • Transcription Factor Targeted Library
  • Peptide Library

生物活性

DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway[1].

IC50 Target

GADD45β/MKK7[1]

体外研究
(In Vitro)

DTP3 (10 μM; 1-21 days) causes the potent and tumor-selective induction of JNK activation and apoptosis, as shown by the appearance of phosphorylated JNK, as early as 24 hours[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: Multiple myeloma (MM) cell lines
Concentration: 10 μM
Incubation Time: 1, 3, 5, 14, 21 days
Result: Caused the appearance of phosphorylated JNK, as early as 24 hours.

体内研究
(In Vivo)

DTP3 TFA (s.c.; 14.5 mg/kg/day; 28 days) has shown a dramatic shrinkage of the tumors, and virtually eradicates established subcutaneous myeloma xenografts in mice[2].
DTP3 TFA (intravenous injection; 10 mg/kg/day) has t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6 to 8-week old male NOD/SCID mice (NOD.CB17-Prkdcscid/IcrCrl; Charles River)[2]
Dosage: 14.5 mg/kg
Administration: S.c.; daily; 28 days
Result: Had shown a dramatic shrinkage of the tumors.
Animal Model: CD1 male mice of 25-30 g[2]
Dosage: 10 mg/kg (Pharmacokinetic Study)
Administration: Intravenous injection
Result: Had t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg.

分子量

639.62

Formula

C28H36F3N7O7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro:;

H2O : 100 mg/mL (156.34 mM; Need ultrasonic)

DMSO : 50 mg/mL (78.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5634 mL 7.8171 mL 15.6343 mL
5 mM 0.3127 mL 1.5634 mL 3.1269 mL
10 mM 0.1563 mL 0.7817 mL 1.5634 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: ≥ 2.5 mg/mL (3.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.91 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.91 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 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 (3.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.91 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 MCE 网站选购。
参考文献
  • [1]. Tornatore L, et al. Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7inhibitor and clinical candidate, DTP3. Toxicol Rep. 2019 Apr 19;6:369-379.

    [2]. Tornatore L, et al. Cancer-selective targeting of the NF-κB survival pathway with GADD45β/MKK7 inhibitors. Cancer Cell. 2014 Oct 13;26(4):495-508.

DAMGO (TFA)

DAMGO (TFA); 纯度: 99.76%

DAMGO TFA 是一种选择性的 μ-阿片受体 (μ-OPR) 激动剂,Kd 值为 3.46 nM。

DAMGO (TFA)amp;;

DAMGO (TFA) Chemical Structure

CAS No. : 950492-85-0

规格 价格 是否有货 数量
10;mM;*;1 mL in Water ¥1367 In-stock
1 mg ¥600 In-stock
5 mg ¥990 In-stock
10 mg ¥1700 In-stock
25 mg ¥3700 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

DAMGO (TFA) 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cancer Compound Library
  • Neurotransmitter Receptor Compound Library
  • Peptide Library

生物活性

DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR[1].

分子量

627.61

Formula

C28H36F3N5O8

CAS 号

950492-85-0

Sequence

Tyr-{d-Ala}-Gly-{Me-Phe}-Gly-ol

Sequence Shortening

Y-{d-Ala}-G-{Me-Phe}-G-ol

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

H2O : 125 mg/mL (199.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5933 mL 7.9667 mL 15.9335 mL
5 mM 0.3187 mL 1.5933 mL 3.1867 mL
10 mM 0.1593 mL 0.7967 mL 1.5933 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)。-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]. FEBS Lett. 1995 Jan 2;357(1):93-7. Onogi T, et al. DAMGO, a mu-opioid receptor selective agonist, distinguishes between mu- and delta-opioid receptors around their first extracellular loops.

Caloxin 2A1 TFA

Caloxin 2A1 TFA; 纯度: 99.69%

Caloxin 2A1 TFA 是一种细胞外质膜 Ca2+-ATPase (PMCA) 肽抑制剂。Caloxin 2A1 TFA 不影响基础 Mg2+-ATPase 或 Na+-K+-ATPase。

Caloxin 2A1 TFAamp;;

Caloxin 2A1 TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ¥500 In-stock
5 mg ¥1100 In-stock
10 mg ¥1800 In-stock
25 mg ¥3600 In-stock
50 mg ¥5400 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

Caloxin 2A1 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Membrane Transporter/Ion Channel Compound Library
  • Peptide Library

生物活性

Caloxin 2A1 TFA is an extracellular plasma membrane Ca2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg2+-ATPase or Na+-K+-ATPase[1].

体外研究
(In Vitro)

Caloxin 2A1 TFA inhibits Ca2+-Mg2+-ATPase in human erythrocyte leaky ghosts, but it does not affect basal Mg2+-ATPase or Na+-K+-ATPase in the ghosts or Ca2+-Mg2+-ATPase in the skeletal muscle sarcoplasmic reticulum. Caloxin 2A1 TFA also inhibits Ca2+-dependent formation of the 140-kDa acid-stable acylphosphate[1].
Caloxin 2A1 TFA increases airway smooth muscle cells (ASMCs) apoptosis[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1592.54

Formula

C66H92F3N19O24

Sequence Shortening

VSNSNWPSFPSSGGG-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

DMSO : 100 mg/mL (62.79 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.6279 mL 3.1396 mL 6.2793 mL
5 mM 0.1256 mL 0.6279 mL 1.2559 mL
10 mM 0.0628 mL 0.3140 mL 0.6279 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)。-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 (1.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.57 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 (1.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.57 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 (1.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.57 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 MCE 网站选购。
参考文献
  • [1]. J Chaudhary, et al. Caloxin: a novel plasma membrane Ca2+ pump inhibitor. Am J Physiol Cell Physiol. 2001 Apr;280(4):C1027-30.

    [2]. Yi-fei Chen, et al. Plasma membrane Ca2+-ATPase regulates Ca2+ signaling and the proliferation of airway smooth muscle cells. Eur J Pharmacol. 2014 Oct 5;740:733-41.