Ranirestat (AS-3201) (AS-3201) 有效且具有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,对重组人 AR 的 Ki 为 0.38 nM .
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Ranirestat (AS-3201) is an aldose reductase inhibitor being developed for the treatment of diabetic neuropathy.
[1]. Kurono M, et al. Stereospecific recognition of a spirosuccinimide type aldose reductase inhibitor (AS-3201) by plasma proteins: a significant role of specific binding by serum albumin in the improved potency and stability. Biochem Pharmacol. 2006 Jan 12;7 [2]. Matsumoto T, et al. Improvement of motor nerve conduction velocity in diabetic rats requires normalization of the polyol pathway metabolites flux. J Pharmacol Sci. 2009 Feb;109(2):203-10. [3]. Toyoda F, et al. Effect of ranirestat, a new aldose reductase inhibitor, on diabetic retinopathy in SDT rats. J Diabetes Res. 2014;2014:672590.
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