属性

折光率 1.62
熔点 208-215° C
沸点 506.2° C
溶解性 Soluble in water (200 mg/mL), and DMSO (95 mg/mL). Insoluble in ethanol.
描述

产品介绍 Fasudil, Monohydrochloride Salt is a cell-permeable, selective ROCK inhibitor which induces neuroprotection in vitro. Studies suggest that when acting as a ROCK inhibitor, Fasudil reduces neutrophil transendothelial migration by diminishing cytoskeletal rearrangement of endothelial cells. In addition, Fasudil significantly protects against MeHg-induced axonal degeneration and apoptotic cell death in cultured cortical neurons. Alternate studies show that Fasudil plays an important role in osteoblastic differentiation of stromal cells via increasing the mRNA expression of collagen-I, osteocalcin, and bone morphogenetic protein-2 (BMP-2). Furthermore, noggin, a BMP-2 antagonist can reverse the effects of Fasudil induced mRNA expression of collagen-I and osteocalcin. Upon inhibition of Rho-kinase, Fasudil significantly stimulates FGF-2-induced accumulation of vascular endothelial growth factor (VEGF). Fasudil, Monohydrochloride Salt is an inhibitor of cGKI, MSK1, PKA, PRK2, Rock-2, AMPK, CaMKII, Polycystin-1 and Rsk-1.
别名 盐酸法舒地尔; (5-异喹啉磺酰基)高哌嗪盐酸盐;5-(1-高哌嗪)磺酰基异喹啉盐酸盐;5-(1-Homopiperazinyl)sulfonylisoquinoline Hydrochloride; 1-(5-Isoquinolinesulfonyl)homopiperazine Hydrochloride; HY-10341; HA-1077; AT-877; Fasudil; Fasudil HCl
生化机理 盐酸法舒地尔能抑制ROCK-II，PKA，PKG，PKC和MLCK，Ki分别为0.33 μM，1.6 μM，1.6 μM，3.3 μM和36 μM。
应用 A selective ROCK inhibitor