Epalrestat

Epalrestat is an inhibitor of aldose reductase (IC50s = 0.01 and 0.26 µM for rat lens and human placenta aldose reductase, respectively). It inhibits glucose-induced sorbitol accumulation in isolated rat lens, rat sciatic nerve, and human erythrocytes (IC50s = 1.5, 5, and 1.5 µM, respectively). It decreases high glucose-induced proliferation of vascular smooth muscle cells when used at a concentration of 10 nM and prevents high glucose-induced intracellular NADH/NAD+ increases and membrane-bound PKC activation at 100 nM. Epalrestat (20 and 40 mg/kg) improves motor nerve conduction velocity and decreases sorbitol content in the sciatic nerve and erythrocytes in a rat model of streptozotocin-induced diabetic neuropathy. It also prevents capillary strand formation in a rat model of diabetes-induced retinal microangiopathy when administered at a dose of 50 mg/kg.Formal Name: 5Z-[(2E)-2-methyl-3-phenyl-2-propen-1-ylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. CAS Number: 82159-09-9. Synonyms: ONO-2235. Molecular Formula: C15H13NO3S2. Formula Weight: 319.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 2 mg/ml. lambdamax: 237, 292, 390 nm. SMILES: CC(/C=C1SC(N(CC(O)=O)C\1=O)=S)=C\C2=CC=CC=C2. InChi Code: InChI=1S/C15H13NO3S2/c1-10(7-11-5-3-2-4-6-11)8-12-14(19)16(9-13(17)18)15(20)21-12/h2-8H,9H2,1H3,(H,17,18)/b10-7+,12-8-. InChi Key: CHNUOJQWGUIOLD-NFZZJPOKSA-N.