A potent aldose reductase inhibitor
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Zopolrestat

Item No. 29185

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 20 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    Zopolrestat is a potent inhibitor of aldose reductase (IC50s = 1.9 and 41 nM for the human placenta and rat lens enzymes, respectively).1 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.2 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; Item No. 13104).1 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.3 Zopolrestat also inhibits glyoxalase I (GLOI; Ki = 18 μM).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mylari, B.L., Larson, E.R., Beyer, T.A., et al. Novel, potent aldose reductase inhibitors: 3,4-Dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners. J. Med. Chem. 34(1), 108-122 (1991).

    2. Qiu, L., Cai, C., Zhao, X., et al. Inhibition of aldose reductase ameliorates ethanol‑induced steatosis in HepG2 cells. Mol. Med. Rep. 15(5), 2732-2736 (2017).

    3. Beyer-Mears, A., Mistry, K., Diecke, F.P.J., et al. Zopolrestat prevention of proteinuria, albuminuria and cataractogenesis in diabetes mellitus. Pharmacology 52(5), 292-302 (1996).

    4. Zhai, J., Zhang, H., Zhang, L., et al. Zopolrestat as a human glyoxalase I inhibitor and its structural basis. ChemMedChem 8(9), 1462-1464 (2013).