store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 PKA、PKC、PKG 的 IC50值分别 0.158 μM 和 4.58 μM、12.30 μM、1.650 μM。
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 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Soluble
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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