产品描述
| 熔点 | 248-249° C |
| 溶解性 | Soluble in water (>20 mg/ml), DMSO (~2 mg/ml), methanol, DMF (~2 mg/ml), and PBS, pH 7.2 (~5 mg/ml). |
| 存贮条件 | 储存温度-20°C |
| 应用 |
HA-1077 二盐酸盐已被用于： 舒张悬臂梁 在离体冠状动脉功能评估中的作用 ·以探讨氮杂吲哚-1、法舒地尔对急性缺氧性肺血管收缩 (HPV) |
| 产品介绍 | HA-1077 dihydrochloride has been shown to be a vasodilating agent as well as a potent inhibitor of Rock-2 (Rho-associated Kinase II), cGKI (cGMP-dependent protein kinase), PKA (cAMP-dependent protein kinase), MYLK, and CaMKII. Rho kinase signaling pathways are thought to cause invasion, migration, and proliferation of certain cells. Studies have shown this compound can also inhibit myosin light chain kinase in vitro and suppress cell rounding by myosin light chain phosphorylation. Mechanistic experiments report that HA-1077 inhibits vascular smooth muscle contraction by acting as a calcium channel protein inhibitor. HA-1077 dihydrochloride is an inhibitor of MSK1, PKC, PRK2 and Rsk-2. |
| 生化机理 | HA-1077/法舒地尔是一种 Rho 激酶抑制剂。这种 ROCK 抑制剂能够增加患有阿尔茨海默氏症(AD)的动物的认知缺陷。在人体中，法舒地尔对蛛网膜下腔出血 (SAH) 后脑血管痉挛具有较好的治疗作用。HA-1077 也可作为蛋白激酶的抑制剂，如肌球蛋白轻链激酶和 Rho 相关激酶。因此，它可以阻止肌球蛋白磷酸化。作为细胞内 Ca2+ 拮抗剂抑制血管平滑肌收缩的新型血管扩张剂。 |
| 别名 | 1-（5-异喹啉磺酰基）高哌嗪 二盐酸盐;法舒地尔 二盐酸盐;HA-1077 二盐酸盐;Fasudil 二盐酸;Fasudil dihydrochloride |
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