GSK-25 是一种有效的、选择性的，具有口服活性的 ROCK1 抑制剂 (IC50=7 nM)。GSK-25 对 31 种激酶以及 RSK1 和 p70S6K 保持良好的选择性 (RSK1: IC50=398 nM, p70S6K: IC50=1 μM)。GSK-25 可抑制 P450 (CYP2C9、CYP2D6、CYP3A4的IC50 分别为2.5、5.2、2.5 μM)。
货号:ajcx15366
CAS:874119-56-9
分子式:C24H16Cl2F2N6O
分子量：513.33
溶解度:DMSO: 100 mg/mL (194.81 mM)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 ?M for CYP2C9, CYP2D6, CYP3A4, respectively)[1].

GSK-25 (Rat aorta IC50=256 nM) is profiled in a spontaneously hypertensive rat (SHR) model of hypertension. At 30 mg/kg (p.o.), GSK-25 induces a 25 mmHg (t=3 hours) drop in blood pressure[1].GSK-25 has promising oral bioavailability (49% in male Sprague-Dawley rats and 19% in monkey), good half-life (1.8 hours in rat and 2.2 hours in monkey)[1].

[1]. Sehon CA, et al. Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases. J Med Chem. 2008 Nov 13;51(21):6631-4.