Zopolrestat

• CAT Number: M005467
• CAS Number: 110703-94-1
• Molecular Formula: C19H12F3N3O3S
• Molecular Weight: 419.378
• Purity: ≥95%
• Target: aldose reductase inhibitor
• Storage: -20°C
• IUPAC Name: 2-[4-oxo-3-[[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]methyl]phthalazin-1-yl]acetic acid
• InChI: 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)
• InChIKey: BCSVCWVQNOXFGL-UHFFFAOYSA-N
• SMILES: C1=CC=C2C(=C1)C(=NN(C2=O)CC3=NC4=C(S3)C=CC(=C4)C(F)(F)F)CC(=O)O

Zopolrestat is a aldose reductase inhibitor potentially for the treatment of diabetic nephropathy and diabetes.

Reference

1:Zopolrestat Induced Suicidal Death of Human Erythrocytes. Bouguerra G, Bissinger R, Abbès S, Lang F.Cell Physiol Biochem. 2015;37(4):1537-46. doi: 10.1159/000438521. Epub 2015 Oct 30. PMID: 26512879 Free Article2:Zopolrestat as a human glyoxalase I inhibitor and its structural basis. Zhai J, Zhang H, Zhang L, Zhao Y, Chen S, Chen Y, Peng X, Li Q, Yuan M, Hu X.ChemMedChem. 2013 Sep;8(9):1462-4. doi: 10.1002/cmdc.201300243. Epub 2013 Jul 15. No abstract available. PMID: 23857942 3:Aldose reductase inhibitors zopolrestat and ferulic acid alleviate hypertension associated with diabetes: effect on vascular reactivity. Badawy D, El-Bassossy HM, Fahmy A, Azhar A.Can J Physiol Pharmacol. 2013 Feb;91(2):101-7. doi: 10.1139/cjpp-2012-0232. Epub 2013 Feb 11. PMID: 23458193 4:Aldose reductase inhibitor zopolrestat restores allergic hyporesponsiveness in alloxan-diabetic rats. Carvalho VF, Barreto EO, Serra MF, Cordeiro RS, Martins MA, Fortes ZB, e Silva PM.Eur J Pharmacol. 2006 Nov 7;549(1-3):173-8. Epub 2006 Aug 26. PMID: 16979157 5:Attenuation of ischemia induced increases in sodium and calcium by the aldose reductase inhibitor zopolrestat. Ramasamy R, Liu H, Oates PJ, Schaefer S.Cardiovasc Res. 1999 Apr;42(1):130-9. PMID: 10435004 6:Bioavailability, multiple-dose pharmacokinetics, and biotransformation of the aldose reductase inhibitor zopolrestat in dogs. Schneider RP, Davenport CJ, Hoffmaster KA, Inskeep PB.Drug Metab Dispos. 1998 Nov;26(11):1160-6. PMID: 9806960 Free Article7:Tissue distribution and biotransformation of zopolrestat, an aldose reductase inhibitor, in rats. Schneider RP, Fouda HG, Inskeep PB.Drug Metab Dispos. 1998 Nov;26(11):1149-59. PMID: 9806959 Free Article8:Comparison of the effects of Zopolrestat and Sorbinil on lens myo-inositol influx. Beyer-Mears A, Diecke FP, Mistry K, Cruz E.Pharmacology. 1997 Feb;54(2):76-83. PMID: 9088040 9:Zopolrestat prevention of proteinuria, albuminuria and cataractogenesis in diabetes mellitus. Beyer-Mears A, Mistry K, Diecke FP, Cruz E.Pharmacology. 1996 May;52(5):292-302. PMID: 8807673 10:The Effect of Urinary pH and Flow Rate on the Renal Elimination of Zopolrestat and Zopolrestat Glucuronide in Humans. Inskeep PB, Chin EB, Henry EW, Lazar JD, Conrad K, Reed AE, Ronfeld RA.Am J Ther. 1996 Mar;3(3):219-224. PMID: 11862253