Tolrestat

Tolrestat is an aldose reductase inhibitor (IC₅₀ = 35 nM for the bovine lens enzyme).¹ Dietary administration of tolrestat decreases sciatic nerve galactitol accumulation in a rat model of galactosemia (ED₅₀ = 7.3 mg/kg per day) and sciatic nerve sorbitol accumulation (ED₅₀ = 4.8 mg/kg per day) in a rat model of diabetes induced by streptozotocin (STZ; Item No. 13104). It also decreases urinary total protein exretion in a rat model of STZ-induced diabetes when administered at a dose of 25 mg/kg per day.² Topical administration of tolrestat (2 and 3% in 10 μl four times per day) decreases levels of galactitol in the lens of and inhibits cataract formation in rats fed a high-galactose diet.³

WARNING This product is not for human or veterinary use.

1. Sestanj, K., Bellini, F., Fung, S., et al. N-[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]- N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor. J. Med. Chem. 27(3), 255-256 (1984).

2. McCaleb, M.L., McKean, M.L., Hohman, T.C., et al. Intervention with the aldose reductase inhibitor, tolrestat, in renal and retinal lesions of streptozotocin-diabetic rats. Diabetologia 34(10), 695-701 (1991).

3. Banditelli, S., Boldrini, E., Vilardo, P.G., et al. A new approach against sugar cataract through aldose reductase inhibitors. Exp. Eye Res. 69(5), 533-538 (1999).