购物车
- 全部删除
- 您的购物车当前为空
Fasudil hydrochloride (HA-1077) 是一种非特异性RhoA/ROCK 抑制剂,也抑制蛋白激酶,对 ROCK1、PKA、PKC 和 MLCK 的 Ki 值分别为 0.33 μM、1.0 μM、9.3 μM 和 55 μM。
Fasudil hydrochloride (HA-1077) 是一种非特异性RhoA/ROCK 抑制剂,也抑制蛋白激酶,对 ROCK1、PKA、PKC 和 MLCK 的 Ki 值分别为 0.33 μM、1.0 μM、9.3 μM 和 55 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50 mg | ¥ 248 | 现货 | |
100 mg | ¥ 428 | 现货 | |
200 mg | ¥ 591 | 现货 | |
500 mg | ¥ 992 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 148 | 现货 |
产品描述 | 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. |
靶点活性 | MLCK:55 μM(ki), ROCK1:0.33 μM(ki), PKA:1.0 μM(ki), PKC:9.3 μM(ki) |
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。 |
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. |
别名 | 盐酸法舒地尔, Fasudil (HA-1077) HCl, HA-1077, Fasudil HCl, HA-1077 hydrochloride, AT-877 |
分子量 | 327.83 |
分子式 | C14H18ClN3O2S |
CAS No. | 105628-07-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 32.8 mg/mL (100 mM) DMSO: 60 mg/mL (183.02 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.