Ranirestat (C09-1167-953)

Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC 50 s of 11 nM and 15 nM for rat lens AR and recombinant human AR , respectively, and a K i of 0.38 nM for recombinant human AR . Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinasIn VitroRanirestat concentration-dependently inhibits sorbitol accumulation in rat erythrocytes and sciatic nerves incubated in the high concentration (500 mg/dl) of glucose. The potency of Ranirestat inhibition of sorbitol accumulation is similar between rat erythrocytes and sciatic nerves with IC 50 values of 0.010 μM and 0.041 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoRanirestat (0.03-1.0 mg/kg; oral administration; once daily; for 3 weeks; male STD-Wistar rats) treatment dose-dependently decreases the elevated sorbitol and fructose levels in the rat sciatic nerves without affecting blood glucose level. Ranirestat also improves the STZ-induced decrease in motor nerve conduction velocity (MNCV) in a dose-dependent manner . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male STD-Wistar rats aged about (12-week-old; 260-290 g) injected with Streptozotocin (STZ) Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg Administration: Oral administration; once daily; for 3 weeks Result: Dose-dependently decreased the elevated sorbitol and fructose levels in the rat sciatic nerves without affecting blood glucose level.IC50& Target:IC50: 11 nM (Rat lens aldose reductase) and 15 nM (Recombinant humanaldose reductase), Ki: 0.38 nM (Recombinant humanaldose reductase). Specification: 10mM in DMSO Molecular Formula: C17H11BrFN3O4 Molecular Weight: 420.19