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| 品牌 | absin | CAS | 105628-07-7 |
|---|---|---|---|
| 分子式 | C14H18ClN3O2S | 纯度 | ＞98% |
| 分子量 | 327.83 | 货号 | abs812079 |
| 规格 | 200mg | 供货周期 | 现货 |
| 主要用途 | 能抑制ROCK-II,PKA，PKG，PKC和MLCK | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Fasudil hydrochloride 105628-07-7
| 产品描述 | |
| 描述 | Fasudil Hydrochloride (盐suan法舒地尔; HA-1077; AT-877) 能抑制ROCK-II，PKA，PKG，PKC和MLCK，Ki分别为0.33 μM，1.6 μM，1.6 μM，3.3 μM和36 μM。 |
| 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 | 盐suan法舒地尔；HA-1077; AT-877; Fasudil HCl |
| 外观 | 白色或类白色结晶性粉末 |
| 可溶性/溶解性 | Water ：65 mg/mL (198.27 mM) DMSO ：5 mg/mL (15.25 mM) Ethanol ：Insoluble |
| 生物活性 | |
| 靶点 | ROCK2 ,PKA ,PKG ,PKC |
| In vitro(体外研究) | Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit 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. 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 suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK. |
| In vivo(体内研究) | Intra-coronary injection of Fasudil to dogs (30 μg i.a.) produces an approximate 50% increase in CBF. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) dose-dependently decreases MBP and increases HR, VBF, CBF, RBF, and FBF. A total dose of 1.0 ng/mL Fasudil increases cardiac output. The infusion of Fasudil 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 significant changes in right atrial pressure, dP/dt or left ventricular minute work in dogs. Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice. |
| 参考文献 | |
| 参考文献 |
| 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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