A potent aldose reductase inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

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 (Request formulation change)
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
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $36

    Add

    5 mg

    $128

    Add

    10 mg

    $236

    Add
    Cayman Chemical
    Explore Obesity & Metabolic Disease Resources

    Discover high-quality research tools to investigate GLP-1 mechanisms and next-generation metabolic targets.

    OBESITY RESEARCH SOLUTIONS
    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).