GSK-25

小分子

GSK-25

G655933-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor ( IC 50 =7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC 50 =398 nM, p70S6K: IC 50 =1 μM). GSK-25 inhibits P450 profile (IC 50 s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) In Vivo GSK-25 (Rat aorta IC 50 =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 . 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:ROCK1 7 nM (IC 50 ) RSK1 398 nM (IC 50 ) p70S6K 1000 nM (IC 50 )

GSK-25 是一种强效、选择性和口服生物利用度高的 ROCK1 抑制剂（IC 50 =7 nM）。GSK-25 对 31 种激酶（>100 倍）以及 RSK1 和 p70S6K 都具有良好的选择性（RSK1：IC 50 =398 nM，p70S6K：IC 50 =1 μM）。GSK-25 可抑制 P450

874119-56-9(DMSO)

C24H16Cl2F2N6O

513.33 g/mol

CC1=C(C(N=C(N1)C2=CC(=NC=C2)Cl)C3=C(C=C(C=C3)Cl)F)C(=O)NC4=C(C=C5C(=C4)C=NN5)F