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Azaindole 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Azaindole 1图片
CAS NO:867017-68-3
规格:98%
分子量:402.79
包装与价格:
包装价格(元)
200mg电议
500mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Azaindole 1是有口服活性,ATP-竞争型的 ROCK 抑制剂,对ROCK-1 和 ROCK-2 的 IC50 值分别为0.6 和 1.1 nM。
CAS:867017-68-3
分子式:C18H13ClF2N6O
分子量:402.79
纯度:98%
存储:Store at -20°C

Background:

Azaindole 1 is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively. ROCK-1|0.6 nM (IC50)|ROCK-2|1.1 nM (IC50)|TRK|252 nM (IC50)|FLT3|303 nM (IC50)


Azaindole 1 is a highly potent inhibitor of human ROCK-1 and ROCK-2, with IC50s of 0.6 and 1.1 nM, respectively, and also inhibits murine ROCK-2 or rat ROCK-2 with IC50s of 2.4 and 0.8 nM, respectively. Azaindole 1 also inhibits receptor tyrosine kinases TRK and FLT3, with IC50s of 252 and 303 nM, respectively, but shows slight inhibition of MLCK and ZIP-kinase with IC50s of 7.4 μM and 4.1 μM, respectively. Azaindole 1 induces vasorelaxation in vitro, and suppresses the phenylephrine-induced contraction of rabbit saphenous artery in a concentration dependent manner with an IC50 value of 65 nM[1].


Azaindole 1 (0.03, 0.1, 0.3 mg/kg, i.v.) results in a dose-dependent and long-lasting decrease in blood pressure in anaesthetized normotensive rats. Azaindole 1 (3 and 10 mg/kg, p.o.) decreases blood pressure dose-dependently and persistently both in normotensive and hypertensive rats, and shows such effects even at 1 mg/kg in hypertensive rats. Azaindole 1 (0.1 and 0.3 mg/kg, i.v. bolus injections) causes decreased mean arterial blood pressure in a dose-related manner and only leads to a moderate and dose-independent increase in heart rate of anaesthetized dogs[1].


[1]. Kast R, et al. Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br J Pharmacol. 2007 Dec;152(7):1070-80. Epub 2007 Oct 15.