Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μ ;M, 1.650 μM 分别代表 ROCK2 和 PKA、PKC、PKG。 HA-1077 (hydrochloride) 也是一种有效的 Ca2+ 通道拮抗剂和血管扩张剂。
| Cas No. | 203911-27-7 |
| 别名 | 盐酸法舒地尔,HA-1077 dihydrochloride; AT-877 dihydrochloride |
| Canonical SMILES | O=S(C1=CC=CC2=CN=CC=C21)(N3CCNCCC3)=O |
| 分子式 | C14H17N3O2S•2HCl |
| 分子量 | 364.3 |
| 溶解度 | DMF: 2 mg/ml,DMSO: 3 mg/ml,PBS (pH 7.2): 5 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Rho-associated kinase (ROCK), an effector of the small GTP-binding protein Rho, plays an important role in various cellular functions including vascular smooth muscle contraction, proliferation, and migration as well as inflammatory cell mobility. HA-1077 is a potent inhibitor of ROCK-II and additionally inhibits protein kinase c-related kinase 2 (PRK2), mitogen- and stress-activated protein kinase (MSK1), and mitogen activated protein kinase-activated protein kinase 1b (MAPKAP-K1b) with IC50 values of 1.9, 4, 5, and 15 µM, respectively. By inhibiting the activity of ROCK, HA-1077 has been shown to reduce blood vessel constriction, decrease pulmonary arterial pressure, inhibit tumor angiogenesis, and improve insulin signaling in various rodent models. While originally marketed for the prevention of cerebral vasospasm in patients with subarachnoid hemorrhage, oral formulations of HA-1077 are used for the treatment of a wide range of cardiovascular diseases including pulmonary arterial hypertension and stable angina. |
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