155558-32-0
155558-32-0 结构式
基本信息
1-羟基法舒地尔
RHO-激酶抑制剂
羟基法舒地尔盐酸盐
1-(1-羟基-5-异喹啉磺酰基)高哌嗪盐酸盐
Hydroxyfasudil HCl
Fasudil Impurity 7 HCl
Hydroxyfasudil (HA-1100)
Hydroxyfasudil Hydrochloride
Hydroxyfasudil (HA-1100) HCl
HYDROXYFASUDIL MONOHYDROCHLORIDE
Hydroxyfasudil hydrochloride hydrate
Hydroxyfasudil - CAS 155558-32-0 - Calbiochem
5-(1,4-diazepan-1-ylsulfonyl)-2h-isoquinolin-1-one
物理化学性质
常见问题列表
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ROCK2 0.72 μM (IC 50 ) |
ROCK1 0.73 μM (IC 50 ) |
PKA 37 μM (IC 50 ) |
Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC 50 s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Hydroxyfasudil also less potently inhibits PKA, with an IC 50 of 37 μM, 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC 50 value of 0.8 ± 0.3 μM. Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours, but does not affect eNOS promoter activity at concentrations from 0.1 to 100 μM.
Hydroxyfasudil (10 mg/kg, i.p.) significantly increases both the average and maximal voided volumes in SD rats. Hydroxyfasudil also significantly decreases the maximal detrusor pressure. Hydroxyfasudil (3 mg/kg, i.p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs). Furthermore, Hydroxyfasudil (3, 10 mg/kg, i.p) significantly ameliorates decreased penile cGMP contents in rats.