Application
一种具有选择性和抗高血压活性的Rho激酶抑制剂。
SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. SAR407899 is equipotent against human and rat-derived Rho-kinase 2 with inhibition constant values of 36 nM and 41 nM, respectively. SAR407899 is approximately 8-fold more active than fasudil. SAR407899 potently (mean IC(50) values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds. The antihypertensive effect of SAR407899 was superior to that of fasudil and Y-27632.
SAR407899有效抑制内皮素1诱导的肾抵抗性动脉收缩。 SAR407899与人和大鼠的Rho激酶2等价,抑制常数分别为36 nM和41 nM。 SAR407899的活性比法舒地尔高约8倍。 SAR407899有效(平均IC(50)值:122至280 nM)和独立于物种的不同物种和不同血管床的预收缩孤立动脉。 SAR407899的抗高血压作用优于法舒地尔和Y-27632。
性质
Iupac Name | 6-(piperidin-4-yloxy)isoquinolin-1-ol |
Inchi Code | 1S/C14H16N2O2/c17-14-13-2-1-12(9-10(13)3-8-16-14)18-11-4-6-15-7-5-11/h1-3,8-9,11,15H,4-7H2,(H,16,17) |
Inchi Key | IPEXHQGMTHOKQV-UHFFFAOYSA-N |
安全信息
RIDADR NONH for all modes of transport