For research use only. Not Intended for Therapeutic Use!
|IC50:||0.33 μM(for ROCK-II)|
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Fasudil Hcl(HA-1077; AT-877) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.
IC50 Value: 0.33 μM(for ROCK-II)
Target: ROCK II; PKC
in vitro: Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. Fasudil induces disorganization of actin stress fiber and cell migration inhibition. Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK.
in vivo: The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice.
. 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.