Hydroxyfasudil, 5 mg

Background: Rho kinase inhibitor. Active metabolite of fasudil (HA-1077). Exists in two tautomers. Hydroxyfasudil relaxes the rabbit basilar artery mainly by disinhibiting myosin light chain phosphatase through the inhibition of rho-associated kinase. The hydroxyfasudil-sensitive Rho-kinase-mediated pathway appears to mediate enhanced myosin light chain  phosphorylations and plays a central role in the pathogenesis of coronary artery spasm.

Chemical formula: C14H17N3O3S . HCl
Molecular weight: 343.8 g/mol
Purity: >98%
Form: solid
Solubility: soluble in water
CAS number: 155558-32-0

Product specific literature references:

Shimokawa H, Seto M, Takeshita A et al. (1999) "Rho-kinase-mediated pathway induces enhanced myosin light chain phosphorylations in a swine model of coronary artery spasm" Cardiovasc Res. 43(4):1029-39

Utsunomiya T, Satoh S, Shimokawa H et al. (2001) "Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a canine model of effort angina" Br J Pharmacol. 134(8):1724-30

Nakamura K, Nishimura J, Kanaide H et al. (2001) "Hydroxyfasudil, an active metabolite of fasudil hydrochloride, relaxes the rabbit basilar artery by disinhibition of myosin light chain phosphatase" J Cereb Blood Flow Metab. 21(7):876-85

Kandabashi T, Shimokawa H, Takeshita A et al. (2002) "Involvement of rho-kinase in agonists-induced contractions of arteriosclerotic human arteries" Arterioscler Thromb Vasc Biol. 22(2):243-8

Takemoto M, Sun J, Hiroki J, Shimokawa H, Liao JK (2002) "Rho-kinase mediates hypoxia-induced downregulation of endothelial nitric oxide synthase" Circulation 106(1):57-62

Yada T, Shimokawa H, Kajiya F et al. (2005) "Beneficial effect of hydroxyfasudil, a specific Rho-kinase inhibitor, on ischemia/reperfusion injury in canine coronary microcirculation in vivo" J Am Coll Cardiol. 45(4):599-607