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Fasudil

Fasudil

产品编号 T1606   CAS 103745-39-7
别名: HA-1077, AT877, 法舒地尔

Fasudil (HA-1077) 是一种非特异性 RhoA/ROCK 抑制剂,也是 Ca2+通道拮抗剂和血管扩张剂。它对蛋白激酶有抑制作用,ROCK1 的 Ki 值为 0.33 μM,ROCK2 和 PKAPKC、PKG 的 IC50值分别 0.158 μM 和 4.58 μM、12.30 μM、1.650 μM。

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Fasudil Chemical Structure
Fasudil, CAS 103745-39-7
规格 价格/CNY 货期 数量
25 mg ¥ 198 现货
50 mg ¥ 276 现货
100 mg ¥ 392 现货
200 mg ¥ 566 现货
500 mg ¥ 968 现货
产品目录号及名称: Fasudil (T1606)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.
靶点活性 ROCK1:0.33 μM(Ki), PKC:9.3 μM(Ki), PKA:1.0 μM(Ki), MLCK:55 μM(Ki)
体外活性 Fasudil (Hydrochloride) has vasodilatory action and occupies the adenine pocket of the ATP-binding site of the enzyme[1]. 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[2]. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction[3]. Fasudil induces disorganization of actin stress fiber and cell migration inhibition[4]. 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[5].
体内活性 Fasudil (30 μg) produces an approximate 50% increase in CBF via intra-coronary injection to dogs. 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[3]. Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[6]. 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[7].
激酶实验 Cyclic AMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HCl (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cyclic AMP or absence of cyclic AMP, 3.3 to 20 μM [r-32P] ATP (4×105 c.p.m.), 0.5 μg of the enzyme, 100 μg of histone H2B and compound. The mixture is incubated at 30°C for 5 min. The reaction is terminated by adding 1mL of ice-cold 20% trichloroacetic acid after adding 500 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 r.p.m. for 15min, the pellet is resuspended in ice-cold 10% trichloro-acetic acid solution and the centrifugation-resuspension cycle is repeated three times. The final pellet is dissolved in 1 mL of 1 N NaOH and radioactivity is measured with a liquid scintillation counter[1].
别名 HA-1077, AT877, 法舒地尔
分子量 291.37
分子式 C14H17N3O2S
CAS No. 103745-39-7

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: Soluble

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Ono-Saito N, et al. H-series protein kinase inhibitors and potential clinical applications. Pharmacol Ther. 1999 May-Jun;82(2-3):123-31. 2. Asano T, et al. Mechanism of action of a novel antivasospasm drug, HA1077. J Pharmacol Exp Ther. 1987 Jun;241(3):1033-40. 3. Asano T, et al. 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. 4. Negoro N, et al. The kinase inhibitor fasudil (HA-1077) reduces intimal hyperplasia through inhibiting migration and enhancing cell loss of vascular smooth muscle cells. Biochem Biophys Res Commun. 1999 Aug 19;262(1):211-5. 5. Fukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25(4):829-38.
[Ala113]-MBP (104-118) acetate CGP 53353 6-Deoxyisojacareubin SAMβA TFA Pep2m, myristoylated acetate Verbascoside Malantide acetate(86555-35-3 free base) HA-1004 dihydrochloride

相关化合物库

该产品包含在如下化合物库中:
自噬库 离子通道库 抑制剂库 上市药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Fasudil 103745-39-7 Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling Membrane transporter/Ion channel Metabolism Stem Cells Tyrosine Kinase/Adaptors ROCK Serine/threonin kinase Calcium Channel PKA PKC LPA ROK Protein kinase C human HSC Inhibitor ERK1/2 AT-877 vasodilator Rho-associated kinase HA-1077 AT877 HA 1077 inhibit TIMP-1 法舒地尔 AT 877 HA1077 protein kinases lysophoaphatidic acid JNK rat HSCs collagen Ca2+ channel antagonist TWNT-4 cells Rho-associated protein kinase orally active Rho-kinase Protein kinase A Ca channels a-SMA p38 Ca2+ channels inhibitor

 

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