tcsc2040 Tolrestat

Tolrestat is a potent, orally active aldose reductase inhibitor with IC₅₀ of 35 nM.

IC50 & Target: IC50: 35 nM (Aldose Reductase)

In Vivo: Tolrestat (1.8 mg/kg per day) causes a reversal to normal RBC sorbitol levels diabetic rats^[1]. In 21-day diabetic rats, the estimated ID in the sciatic nerve and lenses is 4.8 and about 20 for tolrestat, and 1.7 and 2.2 for (±)sorbinil,

respectively^[2]. Either tolrestat or sorbinil inhibits tissue AR activity but does not significantly affect plasma lipoprotein levels, or affect the body weight of the mice or their general health. Accumulation of cholesterol-rich foam cells is significantly increased in aortic roots of tolrestat-fed mice^[3].