Fasudil

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Fasudil

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

103745-39-7

包装与价格：

包装	价格(元)
200mg	询价
500mg	询价

Fasudil (HA-1077; AT877) 是一种非特异性 RhoA/ROCK 抑制剂，对蛋白激酶也有抑制作用，对 ROCK1 的 Ki 为 0.33 μM，对 ROCK2 和 PKA 的 IC50 分别为 0.158 μM 和 4.58 μM、12.30 μM、1.650 μM ，PKC，PKG，分别。 Fasudil 也是一种有效的 Ca2+ 通道拮抗剂和血管扩张剂。

Cas No.	103745-39-7
别名	法舒地尔; HA-1077; AT877
化学名	5-((1,4-diazepan-1-yl)sulfonyl)isoquinoline
Canonical SMILES	O=S(C1=CC=CC2=CN=CC=C21)(N3CCCNCC3)=O
分子式	C₁₄H₁₇N₃O₂S
分子量	291.37
溶解度	Soluble in DMSO
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Ki: 0.33 μM for ROCK-II Cerebral vasospasm occurs frequently after subarachnoid hemorrhage (SAH) secondary to rupture of an intracranial aneurysm. The possibility that calcium entry blockers may be effective on a delayed cerebral vasospasm and the effectiveness of intrathecal administration of the calcium antagonist nifedipine and its analog nimodipine on a vasospasm has been shown from a clinical point of view. Fasudil is a class of calcium antagonists different from the calcium entry blockers. In vitro: The inhibitory effects of fasudil on contractile responses to various agonists were examined on strips of rabbit aorta. The concentration-response curves to 5-hydroxytryptamine, prostaglandin F2alpha, histamine, angiotensin II, noradrenaline and dopamine were concentration-dependently shifted to the right in the presence of fasudil [1]. In vivo: Intra-coronary administration of fasudil to dog dose-dependently increased coronary blood flow, with no effect on mean blood pressure or heart rate. Intra-coronary infusion of atropine, diphenhydramine or propranolol did not modify the in vivo coronary vasodilator response to fasudil [1]. Clinical trial: The previous results suggested that fasudil was equally or more effective than nimodipine for the prevention of cerebral vasospasm and subsequent ischemic injury in patients undergoing surgery for SHA [2]. Reference: [1] Asano T, Suzuki T, Tsuchiya M, Satoh S, Ikegaki I, Shibuya M, Suzuki Y, Hidaka H. Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase. Br J Pharmacol. 1989 Dec;98(4):1091-100. [2] Zhao J, Zhou D, Guo J, Ren Z, Zhou L, Wang S, Zhang Y, Xu B, Zhao K, Wang R, Mao Y, Xu B, Zhang X; 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.