- 生物活性
Tolrestat 是一种有效的，可口服的 aldose reductase 抑制剂，IC50 值为 35 nM。
- 靶点
IC50: 35 nM (Aldose Reductase)
- 体内研究
Tolrestat (1.8 mg/kg per day) causes a reversal to normal RBC sorbitol levels diabetic rats. 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. 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.
- 化学性质
结晶，熔点164-165℃。
托瑞司他甲酯(Tolrestat Methyl Ester)：C17H16F3NO3S。熔点109～110℃。
- 醛糖还原酶抑制剂，毒性低。用于治疗和预防糖尿病并发症，如糖尿病性神经病、肾病、白内障、视网膜病等。
