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Tolrestat | Aldose reductase inhibitor

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Catalog #:

Product Description

Tolrestat is a thioamide-based inhibitor of aldose reductase with an IC50 activity of 35 nM. (1) Along with other similar therapies, Tolrestat has implications in the treatment of diabetic complications, such as diabetic neuropathy, in a manner independent of insulin-related control of blood glucose levels. (2)

In rat diabetes models, Tolrestat reduces sorbitol concentrations in the sciatic nerve and eye lens, as well as prevents diabetic retinopathy, cateracts, thickening of the retinal basement membrane, and nerve dysfunction. Additionally, Tolrestat reduces urinary albumin excretion. (3)

Technical information:

Chemical Formula:   C16H14F3NO3S
CAS #:   82964-04-3
Molecular Weight:   357.35
Purity::   > 98%
Appearance:   white
Chemical Name:   2-(6-methoxy-N-methyl-5-(trifluoromethyl)naphthalene-1-carbothioamido)acetic acid
Solubility:   Up to 22 mM in DMSO
Synonyms:   Tolrestat

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


1. Sestanj et al., N-[[5 -(Trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]-N-methylglycine (Tolrestat), a Potent, Orally Active Aldose Reductase Inhibitor. J. Med. Chem. 1984, 27, 255-256. Pubmed ID: 6422042
2. Kador et al., Aldose Reductase Inhibitors: A Potential New Class of Agents for the Pharmacological Control of Certain Diabetic Complications. J. Med. Chem. 1985, 28(7), 841-849. Pubmed ID: 3925146
3. Fruncillo et al., Pharmacokinetics of the aldose reductase inhibitor tolrestat: Studies in healthy young and elderly male and female subjects and in subjects with diabetes. Clin. Pharmcol. Ther. 1996, 59(6), 602-613. Pubmed ID: 8681485

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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