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| 品牌 | absin | CAS | 103745-39-7 |
|---|---|---|---|
| 分子式 | C14H17N3O2S | 纯度 | ≥98% |
| 分子量 | 291.37 | 货号 | abs812829 |
| 规格 | 250mg | 供货周期 | 现货 |
| 主要用途 | is a potent Rho-kinase inhibitor and va | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Fasudil 103745-39-7
| 产品描述 | |
| 描述 | Fasudil hydrochloride (INN) is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, as well as to improve the cognitive decline seen in stroke victims. It has been found to be effective for the treatment of pulmonary hypertension. |
| 纯度 | ≥98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 法舒地尔；HA-1077；AT877 |
| 外观 | 白色粉末 |
| 可溶性/溶解性 | 10 mM in DMSO |
| 生物活性 | |
| 靶点 | PKA |
| In vitro(体外研究) | Fasudil has vasodilatory action and occupies the adenine pocket of the ATP-binding site of the enzyme. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil inhibits contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. In addition, Fasudil induces disorganization of actin stress fiber and cell migration inhibition. Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil also blocks the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK. |
| In vivo(体内研究) | Fasudil (30 μg) increases CBF by 50% via intra-coronary injection to dogs. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) decreases MBP and increases HR, VBF, CBF, RBF, and FBF. Fasudil (1.0 ng/mL) increases cardiac output. Fasudil via i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without obvious effect on right atrial pressure, dP/dt or left ventricular minute work in dogs. Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. Fasudil (100 mg/kg/day, p.o.) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Fasudil inhibits the proliferative response of splenocytes to the antigen in mice. Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice via p.o. administration. |
| 参考文献 | |
| 参考文献 | 1. Hu H, et al. Exp Mol Pathol. 2015 Apr;98(2):277-85. |
| 研究领域 | |
| 研究领域 | CancerSignal transductionProtein phosphorylationSerine/threonine kinasesOther ApoptosisIntracellularKinases Signal TransductionProtein PhosphorylationSer / Thr KinasesOther Kinases Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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