Cayman Epalrestat

Epalrestat is an inhibitor of aldose reductase (IC₅₀s = 0.01 and 0.26 µM for rat lens and human placenta aldose reductase, respectively).¹ It inhibits glucose-induced sorbitol accumulation in isolated rat lens, rat sciatic nerve, and human erythrocytes (IC₅₀s = 1.5, 5, and 1.5 µM, respectively). It decreases high glucose-induced proliferation of vascular smooth muscle cells when used at a concentration of 10 nM and prevents high glucose-induced intracellular NADH/NAD⁺ increases and membrane-bound PKC activation at 100 nM.^2,3 Epalrestat (20 and 40 mg/kg) improves motor nerve conduction velocity and decreases sorbitol content in the sciatic nerve and erythrocytes in a rat model of streptozotocin-induced diabetic neuropathy.⁴ It also prevents capillary strand formation in a rat model of diabetes-induced retinal microangiopathy when administered at a dose of 50 mg/kg.⁵

WARNING This product is not for human or veterinary use.