货号:A105790 同义名: GSK269962 hydrochloride;GSK269962B
GSK269962A HCl是一种选择性的 ROCK(Rho 相关蛋白激酶)抑制剂,对 ROCK1 和 ROCK2 的 IC50 值分别为 1.6 nM 和 4 nM。
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产品名称 | ROCK ↓ ↑ | ROCK1 ↓ ↑ | ROCK2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Thiazovivin |
+
ROCK, IC50: ~0.5 μM |
98% | |||||||||||||||||
Netarsudil hydrochloride |
++++
ROCK, Ki: 2 nM |
99%+ | |||||||||||||||||
Y-33075 2HCl |
++++
ROCK, IC50: 3.6 nM |
99%+ | |||||||||||||||||
ROCK1-IN-1 |
++
ROCK, Ki: 17nM |
95% | |||||||||||||||||
GSK429286A |
+++
ROCK1, IC50: 14 nM |
++
ROCK2, IC50: 63 nM |
99%+ | ||||||||||||||||
Ripasudil |
++
ROCK1, IC50: 51 nM |
++
ROCK2, IC50: 19 nM |
99%+ | ||||||||||||||||
Belumosudil |
++
ROCK2, IC50: 60 nM ROCK2, Ki: 41 nM |
99%+ | |||||||||||||||||
Y-27632 dihydrochloride |
++
ROCK1, Ki: 140 nM |
+
ROCK2, Ki: 300 nM |
99%+ | ||||||||||||||||
Fasudil HCl |
+
ROCK2, Ki: 330 nM |
PKG,Rho | 98% | ||||||||||||||||
Chroman 1 |
++++
ROCK1, IC50: 52 pM |
++++
ROCK2, IC50: 1 pM |
99% | ||||||||||||||||
BAY-549 |
++++
ROCK1, IC50: 0.6 nM |
++++
ROCK2, IC50: 1.1 nM |
99%+ | ||||||||||||||||
AT13148 |
+++
ROCK1, IC50: 6 nM |
+++
ROCK2, IC50: 4 nM |
PKA | 98+% | |||||||||||||||
RKI-1447 |
+++
ROCK1, IC50: 14.5 nM |
+++
ROCK2, IC50: 6.2 nM |
99%+ | ||||||||||||||||
Hydroxyfasudil HCl |
+
ROCK1, IC50: 0.73 μM |
+
ROCK2, IC50: 0.72 μM |
PKA | 99% | |||||||||||||||
H-1152 2HCl |
+++
ROCK2, IC50: 0.0120 μM |
PKG | 99% | ||||||||||||||||
GSK269962A HCl |
++++
ROCK1, IC50: 1.6 nM |
+++
ROCK2, IC50: 4 nM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | GSK269962A (GSK 269962) is a potent ROCK inhibitor, which effective against both ROCK1 and ROCK2 isoforms, with IC50 values of 1.6 and 4 nM, respectively. GSK269962A has anti-inflammatory and vasodilatory activities[1]. |
体内研究 | GSK269962A, administered via oral gavage at doses of 0.3, 1, and 3 mg/kg, leads to a dose-dependent and significant reduction in blood pressure in spontaneously hypertensive rats (SHR), indicating its potential in managing hypertension[1]. |
体外研究 | GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM[1]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
697 cell | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay, IC50=0.2991 μM | SANGER | ||
8-MG-BA cell | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.0793 μM | SANGER | ||
A101D cell | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50=1.87034 μM | SANGER | ||
ACN cell | Growth inhibition assay | Inhibition of human ACN cell growth in a cell viability assay, IC50=21.4387 μM | SANGER | ||
Dose | Rat: 30 mg/kg[2] (i.v.); 1 mg/kg- 30 mg/kg[3] (p.o.); 5 mg/kg, 10 mg/kg[4] (intra-arterially) |
Administration | i.v., p.o., intra-arterially |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.65mL 0.33mL 0.16mL |
8.24mL 1.65mL 0.82mL |
16.47mL 3.29mL 1.65mL |
CAS号 | 2095432-71-4 |
分子式 | C29H31ClN8O5 |
分子量 | 607.06 |
别名 | GSK269962 hydrochloride;GSK269962B;GSK269962;GSK269962A hydrochloride |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,2-8°C |
溶解度 | |
动物实验配方 |
IP 2% DMSO+water 0.7 mg/mL clear PO 0.5% CMC-Na 40 mg/mL suspension |