羟基法舒地尔
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- CAS号:
- 105628-72-6
- 英文名:
- 1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE
- 英文别名:
- Ha 1100;Fasudil Impurity L;Fasudil Impurity 5;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-diazepan-1-yl)sulfonyl)isoquinolin-1(8aH)-one
- 中文名:
- 羟基法舒地尔
- 中文别名:
- 法舒地尔23;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-((1,4-二氮杂环庚烷-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
- CBNumber:
- CB7847446
- 分子式:
- C14H17N3O3S
- 分子量:
- 307.37
- MOL File:
- 105628-72-6.mol
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羟基法舒地尔化学性质
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储存条件:
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Sealed in dry,Store in freezer, under -20°C
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溶解度:
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Soluble in DMSO
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羟基法舒地尔性质、用途与生产工艺
Hydroxyfasudil 是一种 ROCK 抑制剂，可抑制 ROCK1 和 ROCK2 的活性，IC50 值分别为 0.73 和 0.72 μM。
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ROCK2
0.72 μM (IC
50
)
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ROCK1
0.73 μM (IC
50
)
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PKA
37 μM (IC
50
)
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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.
羟基法舒地尔
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105628-72-6, 羟基法舒地尔 相关搜索:
- Intracellular signaling
- Angiogenesis and Metastasis
- 药靶配体
- 细胞周期
- C14H17N3O3S
- 法舒地尔23
- 5-((1,4-二氮杂环庚烷-1-基)磺酰基)异喹啉-1(2H)-酮
- 5-((1,4-二氮杂卓-1-基)磺酰基)异喹啉-1(2H)-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-[(六氢-1H-1,4-二氮杂卓-1-基)磺酰基]-1(2H)-异喹啉酮
- 法舒地尔杂质L
- 105628-72-6
- Fasudil Impurity 5
- HA1100,ROCK,Rho-kinase,inhibit,Rho-associated kinase,Inhibitor,ROK,Hydroxyfasudil,HA 1100,Rho-associated protein kinase
- 5-((1,4-diazepan-1-yl)sulfonyl)isoquinolin-1(8aH)-one
- 1(2H)-Isoquinolinone, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-
- HA-1100;HA 1100;HA1100
- Fasudil impurity 12/5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one hydrochloride
- 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinolin-1(2H)-one
- 1-[(1,2-DIHYDRO-1-OX
- Fasudil Impurity L
- 5-((1,4-diazepan-1-yl)sulfonyl)isoquinolin-1-ol
- HA 1100 HYDROCHLORIDE
- 1-[(1,2-Dihydro-1-oxo-5-isoquinolinyl)sulfonyl]hexahydro-1H-1,4-diazepinehydrochloride
- Hexahydro-1-((1,2-dihydro-1-oxo-5-isoquinolinyl)sulfonyl)-1H-1,4-diazepine
- Ha 1100
- 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-DIAZEPINE
- HYDROXYFASUDIL;HA-1100;HA 1100;HA1100
- 5-(1,4-diazepane-1-sulfonyl)-1,2-dihydroisoquinolin-1-one