Zopolrestat

Zopolrestat is a potent inhibitor of aldose reductase (IC50s = 1.9 and 41 nM for the human placenta and rat lens enzymes, respectively). It inhibits sorbitol accumulation in human and rat erythrocytes (IC50s = 370 and 220 nM, respectively). Zopolrestat (50 µM) inhibits ethanol-induced aldose reductase activity and lipid accumulation in HepG2 cells. In vivo, zopolrestat (50 mg/kg) reduces sciatic nerve, retina, and lens accumulation of sorbitol in a rat model of diabetes induced by streptozotocin (STZ, Cay-13104). It also reduces protein excretion and maintains lens transparency and myo-inositol content, markers of cataract development, in rats with STZ-induced diabetes when administered at a dose of 100 mg/kg. Zopolrestat also inhibits glyoxalase I (GLOI, Ki = 18 µM).Formal Name: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl]methyl]-1-phthalazineacetic acid. CAS Number: 110703-94-1. Molecular Formula: C19H12F3N3O3S. Formula Weight: 419.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 20 mg/ml. lambdamax: 221 nm. SMILES: O=C1C2=CC=CC=C2C(CC(O)=O)=NN1CC3=NC(C=C(C(F)(F)F)C=C4)=C4S3. InChi Code: InChI=1S/C19H12F3N3O3S/c20-19(21,22)10-5-6-15-14(7-10)23-16(29-15)9-25-18(28)12-4-2-1-3-11(12)13(24-25)8-17(26)27/h1-7H,8-9H2,(H,26,27). InChi Key: BCSVCWVQNOXFGL-UHFFFAOYSA-N.