Fasudil

• CAT Number: I000221
• CAS Number: 103745-39-7
• Molecular Formula: C14H17N3O2S
• Molecular Weight: 291.37
• Purity: ≥95%
• Synonyms: 5-((1,4-diazepan-1-yl)sulfonyl)isoquinoline
• Target: ROCK
• Solubility: DMSO 5 mg/mL; Water 65 mg/mL
• Storage: Store at -20C
• IC50: 0.33 μM(for ROCK-II)
• IUPAC Name: 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline
• InChI: InChI=1S/C14H17N3O2S/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14/h1,3-5,7,11,15H,2,6,8-10H2
• InChIKey: NGOGFTYYXHNFQH-UHFFFAOYSA-N
• SMILES: C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3

Fasudil (Cat No.:I000221), also known as Fasudil hydrochloride or HA-1077, is a potent inhibitor of multiple enzymes including ROCK-II (Rho-associated protein kinase II), PKA (protein kinase A), PKG (protein kinase G), PKC (protein kinase C), and MLCK (myosin light-chain kinase). By inhibiting these enzymes, Fasudil modulates various cellular signaling pathways involved in smooth muscle contraction, vasodilation, and cell migration. It has been studied for its therapeutic potential in conditions such as hypertension, cerebral vasospasm, and certain cardiovascular diseases.

Reference

[1]. 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.

[2]. 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.

[3]. 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.

[4]. Saito M, et al. Hydroxyfasudil ameliorates penile dysfunction in the male spontaneously hypertensive rat. Pharmacol Res. 2012 Oct;66(4):325-31.

[5]. 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.