Fasudil Hydrochloride(盐酸法舒地尔, AT-877, AT877, Fasudil HCl, HA1077, Fasudil (HA-1077) HCl, HA 1077 hydrochloride)是一种有效的Rho激酶抑制剂、Ca2+通道拮抗剂和血管扩张剂,其抑制ROCK1的Ki值为0.33 μM,抑制ROCK2的IC50值为0.158 μM,PKA的IC50值为4.58 μM,PKC的IC50值为12.30 μM,PKG的 IC50值1.650 μM。Fasudil Hydrochloride通过增加肌球蛋白轻链磷酸酶的活性来扩张血管,削弱内皮细胞张力,改善脑组织循环,拮抗炎症因子,促进神经再生,是一种具有广泛药理作用的新型药物。
参考文献
[1]. Fukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25(4):829-38.
[2]. Sun X, et al. The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 2006 Nov;180(1-2):126-34. Epub 2006 Sep 22.
[3]. Huang XN, et al. The effects of fasudil on the permeability of the rat blood-brain barrier and blood-spinal cordbarrier following experimental autoimmune encephalomyelitis. J Neuroimmunol. 2011 Oct 28;239(1-2):61-7.
冰袋运输。粉末直接保存于-20℃,有效期2年。建议分装后-20℃干燥保存,避免反复冻融。