中文名 | 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 |
英文名 | Hydroxyfasudil |
别名 | 羟基法舒地尔 法舒地尔杂质L 5-((1,4-二氮杂卓-1-基)磺酰基)异喹啉-1(2H)-酮 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 |
英文别名 | HA1100 HA 1100 HA-1100 Ha 1100 Hydroxyfasudil HYDROXYFASUDIL 5-((1,4-diazepan-1-yl)sulfonyl)isoquinolin-1-ol 5-(1,4-diazepane-1-sulfonyl)-1,2-dihydroisoquinolin-1-one 1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE Hexahydro-1-((1,2-dihydro-1-oxo-5-isoquinolinyl)sulfonyl)-1H-1,4-diazepine 1H-1,4-Diazepine, hexahydro-1-((1,2-dihydro-1-oxo-5-isoquinolinyl)sulfonyl)- 1-[(1,2-Dihydro-1-oxo-5-isoquinolinyl)sulfonyl]hexahydro-1H-1,4-diazepinehydrochloride |
CAS | 105628-72-6 |
化学式 | C14H17N3O3S |
分子量 | 307.37 |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
体外研究 | 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. |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.253 ml | 16.267 ml | 32.534 ml |
5 mM | 0.651 ml | 3.253 ml | 6.507 ml |
10 mM | 0.325 ml | 1.627 ml | 3.253 ml |
5 mM | 0.065 ml | 0.325 ml | 0.651 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!