105628-72-6
105628-72-6 结构式
基本信息
5-[(六氢-1H-1,4-二氮杂卓-1-基)磺酰基]-1(2H)-异喹啉酮
Fasudil Impurity L
1-[(1,2-DIHYDRO-1-OX
HA 1100 HYDROCHLORIDE
HA-1100
HA 1100
HA1100
HYDROXYFASUDIL
HA-1100
HA 1100
HA1100
5-((1,4-diazepan-1-yl)sulfonyl)isoquinolin-1-ol
5-((1,4-Diazepan-1-yl)sulfonyl)isoquinolin-1(2H)-one
5-(1,4-diazepane-1-sulfonyl)-1,2-dihydroisoquinolin-1-one
1(2H)-Isoquinolinone, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-
常见问题列表
|
ROCK2 0.72 μM (IC 50 ) |
ROCK1 0.73 μM (IC 50 ) |
PKA 37 μM (IC 50 ) |
Hydroxyfasudil 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.