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105628-72-6

中文名稱 羥基法舒地爾
英文名稱 1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE
CAS 105628-72-6
分子式 C14H17N3O3S
分子量 307.37
MOL 文件 105628-72-6.mol
更新日期 2025/02/26 11:53:56
105628-72-6 結(jié)構(gòu)式 105628-72-6 結(jié)構(gòu)式

基本信息

中文別名
法舒地爾雜質(zhì)L
5-[(六氫-1H-1,4-二氮雜卓-1-基)磺?;鵠-1(2H)-異喹啉酮
英文別名
Ha 1100
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]-

物理化學(xué)性質(zhì)

儲存條件Sealed in dry,Store in freezer, under -20°C
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
毒性mouse,LD50,unreported,145mg/kg (145mg/kg),United States Patent Document. Vol. #4678783,

常見問題列表

生物活性
Hydroxyfasudil 是一種 ROCK 抑制劑,可抑制 ROCK1 和 ROCK2 的活性,IC50 值分別為 0.73 和 0.72 μM。
靶點(diǎn)

ROCK2

0.72 μM (IC 50 )

ROCK1

0.73 μM (IC 50 )

PKA

37 μM (IC 50 )

體外研究

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.

體內(nèi)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.

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