Hydroxyfasudil HCl (HA1100)

Description: Hydroxyfasudil HCl (also called HA1100 HCl), a metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. It acts as a ROCK inhibitor, with IC50s of 0.73 and 0.72 uM for ROCK1 and ROCK2, respectively. Hydroxyfasudil prevents the downregulation of endothelial NO synthase (eNOS) under hypoxic conditions. In a concentration-dependent manner, hydroxyfasudil increases eNOS mRNA and protein expression, resulting in a 1.9- and 1.6-fold increase, respectively, at 10 umol/L. This correlates with a 1.5- and 2.3-fold increase in eNOS activity and NO production, respectively.

References: Stroke. 2005; 36(10):2251-7; J Am Coll Cardiol. 2005; 45(4):599-607; Br J Pharmacol. 2001; 134(8):1724-30.

Related CAS: 105628-72-6 (free); 155558-32-0 (HCl)