|5-((1,4-二氮杂环庚烷-1-基)磺酰基)异喹啉-1(2H)-酮盐酸盐|CsnPharm

CAS No.: 155558-32-0

Hydroxyfasudil HCl/羟基法舒地尔盐酸盐 Catalog No. CSN15927

Synonyms: HA-1100 hydrochloride;HA-1100 HCl;HA-1100 (hydrochloride)

Hydroxyfasudil HCl, metabolite of fasudil, is a potent Rho-kinase inhibitor and vasodilator.

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技术信息

生物活性

描述Hydroxyfasudil is a hydroxylated metabolite of fasudil hydrochloride, which is a potent inhibitor of ROCK, PKC and MLCK, usually used in the research related to cardiovascular diseases. Hydroxyfasudil elicited a dose-dependent relaxation of the artery accompanied with dephosphorylation of the myosin light chain in a study on intact rabbit basilar artery. This may due to its effect on disinhibiting myosin light chain phosphatase through the inhibition of ROCK depending on the intracellular ATP concentration. Treatment with hydroxyfasudil at concentration ranging in 1-100μM could dose-dependently reverse the decreased eNOS level and its activity caused by hypoxia increased Rho-kinase expression and activity in saphenous vein endothelial cells. Inhibition of ROCK in vivo through administration of hydroxyfasudil at dose of 10mg/kg, i.p., before or immediately after dMCAO (distal middle cerebral artery occlusion), reduced the area of severely ischemic cortex in wild-type and eNOS^-/- mice but did not reduce the area of CBF deficit in eNOS^-/- mice.
动物研究
剂量
Rat: 3 mg/kg, 10 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Rat: 3 mg/kg, 10 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Satoh S, Kawasaki K, Ikegaki I, et al. Evidence of a direct cellular protective effect of Rho-kinase inhibitors on endothelin-induced cardiac myocyte hypertrophy. Biochem Biophys Res Commun. 2012 Jul 27;424(2):338-40.
[2] Zhao J, Zhou D, et al. Fasudil Aneurysmal Subarachnoid Hemorrhage Study Group. Efficacy and safety of fasudil in patients with subarachnoid hemorrhage: final results of a randomized trial of fasudil versus nimodipine. Neurol Med Chir(Tokyo). 2011;51(10):679-83.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9084 mL
- 14.5421 mL
- 29.0842 mL
- 5 mM
- 0.5817 mL
- 2.9084 mL
- 5.8168 mL
- 10 mM
- 0.2908 mL
- 1.4542 mL
- 2.9084 mL

技术信息

CAS号

155558-32-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H18ClN3O3S

运输

蓝冰

分子量

343.83

别名

HA-1100 hydrochloride;HA-1100 HCl;HA-1100 (hydrochloride);Hydroxyfasudil HCl;羟基法舒地尔盐酸盐

溶解度

DMSO	13.94 mg/mL (40.5 mM) warming
Water	8.79 mg/mL (25.6 mM) warming

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Hydroxyfasudil HCl/羟基法舒地尔盐酸盐 Catalog No. CSN15927

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