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CAS No.: 850664-21-0

GSK269962A Catalog No. CSN18470

Synonyms: GSK 269962;GSK269962B

GSK269962A is a potent ROCK inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively), and displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 ROCK1

IC50:1.6nM ROCK2

IC50:4nM
描述GSK269962A can potently inhibit ROCK enzymatic activity with IC50 values of 1.6nM and 4nM for ROCK1 and ROCK2 (measured by purified recombinant protein), respectively, also show inhibition against RSK1 and MSK1 with IC50 values of 132nM and 49nM. Pre-treatment with 3μM GSK269962A 30 minutes before AngII stimulation could inhibit the actin stress fiber formation induced by AngII in human primary aortic smooth muscle cells. Addition with GSK269962A into the tissue bath showed concentration-dependent relaxing effect with IC50 value of 35nM on contracted blood vessels induced by phenylephrine in vitro due to the inhibition of ROCK inhibition by GSK269962A. Oral administration of 0.3-3mg/kg GSK269962A dose-dependently reduced blood pressure in both SHR and DOCA-treated hypertensive rats. GSK269962A at concentration of 50nM could dramatically inhibit basal myometrial contraction at 72h and abolish the procontractile effect of LPS, but appeared to enhance LPS-induced secretion of IL-8 in PHM1-41 cells.
动物研究
剂量
Rat: 0.3 mg/kg - 3 mg/kg^[2] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Rat: 0.3 mg/kg - 3 mg/kg^[2] (p.o.)
给药途径	p.o.

[1] Hutchinson JL, Rajagopal SP, et al. Lipopolysaccharide promotes contraction of uterine myocytes via activation of Rho/ROCK signaling pathways. FASEB J. 2014 Jan;28(1):94-105.
[2] Doe C, Bentley R, et al. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7525 mL
- 8.7627 mL
- 17.5254 mL
- 5 mM
- 0.3505 mL
- 1.7525 mL
- 3.5051 mL
- 10 mM
- 0.1753 mL
- 0.8763 mL
- 1.7525 mL

技术信息

CAS号

850664-21-0

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H30N8O5

运输

蓝冰

分子量

570.60

别名

GSK 269962;GSK269962B

溶解度

DMSO	29.0 mg/mL (50.8 mM)
Water	Insoluble

动物实验配方

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靶点	Description	IC50
ROCK1		IC50:1.6nM
ROCK2		IC50:4nM

GSK269962A Catalog No. CSN18470

靶点选择性

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