For research use only. Not Intended for Therapeutic Use!
|IC50:||0.12 uM (ROCK1); 0.17 uM (ROCK2) |
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Hydroxyfasudil(HA1100), metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.
IC50 Value: 0.12 uM (ROCK1); 0.17 uM (ROCK2) 
in vitro: Fasudil (1-10 μM) and hydroxyfasudil (0.3-10 μM) significantly prevented endothelin-induced cardiomyocyte hypertrophy . Hydroxyfasudil significantly attenuated serotonin (IC)-induced vasoconstriction of SA (-7 +/- 1% vs. 2 +/- 1%, p < 0.01). Coronary I/R significantly impaired coronary vasodilation to acetylcholine after I/R (SA, p < 0.05; and A, p < 0.01 vs. before I/R) and L-NMMA further reduced the vasodilation, whereas hydroxyfasudil completely preserved the responses.
in vivo: Treatment with hydroxyfasudil significantly improved bladder intercontraction intervals. Rats treated with hydroxyfasudil also showed a significant reduction of histopathological features associated with cystitis . Twelve-week-old male SHRs were treated with hydroxyfasudil (3 or 10 mg/kg, i.p.) once a day for 6 weeks. Treatment with hydroxyfasudil significantly improved the decreased penile cGMP concentrations, the increased Rho kinase activities, the increased norepinephrine-induced contractions, and the decreased acetylcholine-induced relaxation in a dose-dependent manner .
Toxicity: The proportion of patients with good clinical outcome was 74.5% (41/55) in the fasudil group and 61.7% (37/60) in the nimodipine group. There were no serious adverse events reported in the fasudil group .
Clinical trial: N/A
. Tsutomu Akama, et al. Linking Phenotype to Kinase: Identification of a Novel Benzoxaborole Hinge Binding Motif for Kinase Inhibition and the Development of High Potency Rho-Kinase Inhibitors. JPET Fast Forward. Published on September 18, 2013.
. Satoh S, et al. Evidence of a direct cellular protective effect of Rho-kinase inhibitors on endothelin-induced cardiac myocyte hypertrophy. Biochem Biophys Res Commun. 2012 Jul 27;424(2):338-40.
. Shimizu N, et al. Effects of the Rho kinase inhibitor, hydroxyfasudil, on bladder dysfunction and inflammation in rats with HCl-induced cystitis. Int J Urol. 2013 Feb 19.
. Saito M, et al. Hydroxyfasudil ameliorates penile dysfunction in the male spontaneously hypertensive rat. Pharmacol Res. 2012 Oct;66(4):325-31.
. Zhao J, et al. Efficacy and safety of fasudil in patients with subarachnoid hemorrhage: final results of a randomized trial offasudil versus nimodipine. Neurol Med Chir (Tokyo). 2011;51(10):679-83.