羟基法舒地尔
中文名称 | 羟基法舒地尔 |
---|---|
中文同义词 | 法舒地尔杂质L;5-[(六氢-1H-1,4-二氮杂卓-1-基)磺酰基]-1(2H)-异喹啉酮;1 - [(1,2-二氢-1-氧代-5-异喹啉基)磺酰基]六氢-1H-1,4-二氮杂盐酸盐;5-((1,4-二氮杂卓-1-基)磺酰基)异喹啉-1(2H)-酮;5-((1,4-二氮杂环庚烷-1-基)磺酰基)异喹啉-1(2H)-酮;法舒地尔23;1-[(1,2-二氢-1-氧代-5-异喹啉YL)磺酰基]六氢-1H-1,4-二氮杂卓 |
英文名称 | 1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE |
英文同义词 | 5-(1,4-diazepane-1-sulfonyl)-1,2-dihydroisoquinolin-1-one;HYDROXYFASUDIL;HA-1100;HA 1100;HA1100;1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE;1H-1,4-Diazepine, hexahydro-1-((1,2-dihydro-1-oxo-5-isoquinolinyl)sulfonyl)-;Ha 1100;Hexahydro-1-((1,2-dihydro-1-oxo-5-isoquinolinyl)sulfonyl)-1H-1,4-diazepine;1-[(1,2-Dihydro-1-oxo-5-isoquinolinyl)sulfonyl]hexahydro-1H-1,4-diazepinehydrochloride;HA 1100 HYDROCHLORIDE |
CAS号 | 105628-72-6 |
分子式 | C14H17N3O3S |
分子量 | 307.37 |
EINECS号 | |
相关类别 | 细胞周期;Angiogenesis and Metastasis;Intracellular signaling |
Mol文件 | 105628-72-6.mol |
结构式 |
羟基法舒地尔 性质
储存条件 | Sealed in dry,Store in freezer, under -20°C |
---|---|
溶解度 | 溶于二甲基亚砜 |
形态 | 固体 |
颜色 | 白色至米白色 |
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.
安全信息
毒性 | mouse,LD50,unreported,145mg/kg (145mg/kg),United States Patent Document. Vol. #4678783, |
---|