Ripasudil (hydrochloride hydrate)

Ripasudil is an inhibitor of Rho-associated kinase 1 (ROCK1) and ROCK2 (IC50s = 51 and 19 nM, respectively). It is selective for ROCK1 and ROCK2 over protein kinase A catalytic subunit alpha (PKACalpha) and PKC (IC50s = 2,100 and >10,000 nM, respectively). Ripasudil (0.4%) reduces intraocular pressure in cynomolgus monkey to a greater extent than the prostaglandin FP receptor agonist latanoprost (Cay-16812). It increases the outflow facility of the aqueous humor in rabbit eyes when administered in a 0.4% solution. Ripasudil (0.4%) decreases intraocular pressure, retinal ganglion cell death, and thinning of inner retinal layers, as well as improves retinal function, in an excitatory amino acid transporter 1 (EAAT1) knockout mouse model of normal tension glaucoma. Formulations containing ripasudil have been used in the treatment of glaucoma and ocular hypertension.Formal Name: 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-isoquinoline, monohydrochloride, dihydrate. CAS Number: 887375-67-9. Synonyms: K-115. Molecular Formula: C15H18FN3O2S . HCl [2H2O]. Formula Weight: 395.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: Slightly soluble, DMSO: 30 mg/ml, PBS (pH 7.2): 0.5 mg/ml. lambdamax: 211, 278, 324 nm. SMILES: FC1=C2C(C=CC=C2S(N3CCCNC[C@@H]3C)(=O)=O)=CN=C1.Cl.O.O. InChi Code: InChI=1S/C15H18FN3O2S.ClH.2H2O/c1-11-8-17-6-3-7-19(11)22(20,21)14-5-2-4-12-9-18-10-13(16)15(12)14,,,/h2,4-5,9-11,17H,3,6-8H2,1H3,1H,2*1H2/t11-,,,/m0.../s1. InChi Key: CMDJNMACGABCKQ-XVSRHIFFSA-N.