147254-64-6 雷尼司他

WGK Germany:WGK 3 存储类别:11 - 可燃固体 危险性类别:眼部刺激 类别2 经皮刺激 类别2 特异性靶器官毒性-一次接触，类别3

• 生物活性 Ranirestat (AS-3201) 是一种有效的，口服活性的醛糖还原酶 (AR) 抑制剂，对大鼠晶状体 AR 和重组人 AR 的 IC50 分别为 11 nM 和 15 nM，对于重组人 AR 的 Ki 为 0.38 nM。Ranirestat 可用于糖尿病感觉运动性多发性神经病的研究，并且对糖尿病视网膜具有神经保护作用。
• 靶点 IC50: 11 nM (Rat lens aldose reductase) and 15 nM (Recombinant humanaldose reductase) Ki: 0.38 nM (Recombinant humanaldose reductase)
• 体外研究 Ranirestat 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.
• 体内研究 Ranirestat (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. 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.

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