| 名称 | Fasudil hydrochloride |
| 描述 | Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively. |
| 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. |
| 体外活性 | 静脉注射0.01,0.03,0.1 和 0.3 mg/kg Fasudil剂量依赖性地降低MBP,提高HR,VBF,CBF,RBF和FBF.总剂量为1.0 ng/mL的 Fasudil提高心脏的输出量.通过冠状动脉内注射给实验狗30 μg Fasudil导致CBF增加约50％.口服Fasudil（剂量为100 mg/kg/天）显著降低用PLP p139-151免疫的SJL/J小鼠中EAE的发病率和平均最大临床评分.Fasudil抑制小鼠脾细胞对抗原的增殖反应.Fasudil处理显示心血管疾病的保护作用,并减少JNK的激活和减少AIF在缺血性损伤下的线粒体核移位. |
| 体内活性 | Fasudil诱导肌动蛋白纤维解体,且抑制细胞迁移。Fasudil竞争性抑制Ca2+诱导的去极化兔主动脉收缩。Fasudil抑制对KCl,血清苯丙氨酸和前列腺素F2a的收缩反应。Fasudil抑制肝星状细胞的扩散,应力纤维的形成和α-SMA的表达,且抑制细胞生长,但不诱导细胞凋亡。Fasudil抑制LPA诱导的ERK1/2,JNK 和 p38 MAPK磷酸化。Fasudil还通过抑制5-羟色胺,去甲肾上腺素,组胺,血管紧张素和多巴胺诱导的螺旋条收缩来发挥血管舒张作用。 |
| 存储条件 | keep away from direct sunlight,keep away from moisture,store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : 32.8 mg/mL (100.05 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (10.07 mM), Sonication is recommended.
DMSO : 82 mg/mL (250.13 mM), Sonication is recommended.
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| 关键字 | TWNT-4 cells | TIMP-1 | threoninkinase | threonin kinase | Serinekinase | Serine kinase | ROCK2 | ROCK | rat HSCs | protein kinases | Protein kinase A | PKG | PKC | PKA | p38 | MLCK | lysophoaphatidic acid | LPA | human HSC | HIVProtease | HIV Protease | HIV | HA1077 Hydrochloride | HA1077 | HA 1077 Hydrochloride | HA 1077 | Fasudil | ERK1/2 | CalciumChannel | Calcium Channel | Ca2+ channel antagonist | Autophagy | AT-877 | AT877 | AT 877 | a-SMA |
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| 相关库 | 神经保护化合物库 | 抑制剂库 | 经典已知活性库 | 抗癌上市药物库 | 激酶抑制剂库 | 抗衰老化合物库 | 离子通道库 | TGF-β/Smad靶点化合物库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | 疼痛相关化合物库 | 抗癌药物库 |