SAR407899 是一种选择性的 ATP 竞争性ROCK抑制剂，对ROCK-2的IC50值为 135 nM，对人和大鼠ROCK-2的Ki值分别为 36 和 41 nM。它是 Rho 激酶抑制剂，有效抑制 endothelin-1 诱导的肾阻力动脉收缩。

SAR407899 is Rho kinase inhibitor potently inhibits endothelin-1-induced constriction of renal resistance arteries.

In vivo, SAR407899 dose-dependently induced rabbit penile erection, with greater potency and longer duration of action than sildenafil[1].

Compared the effects of SAR407899, the Rho-kinase inhibitor Y-27632 and the PDE5 inhibitor sildenafil for their ability to relax corpus cavernosum strips contracted with phenylephrine in healthy and diabetic animals. Strips were obtained from WKY, spontaneous hypertensive (SHR), control CD, and diabetic CD rats, humans, control and diabetic rabbits. Diabetes was induced by streptozotocin or alloxan injection. In vivo penile erection (length) induced by drugs was measured in conscious rabbits[1].

923359-38-0

C14H16N2O2

244.29

DMSO:6 mg/mL (24.56 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years