Ranirestat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC50s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a Ki 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 retinas.

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 IC50 values of 0.010 μM and 0.041 μM, respectively.

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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Endocrinology/Hormones

Reductase

Reductase

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147254-64-6

420.19

C17H11BrFN3O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 50 mg/mL (118.99 mM)

Fc1cc(Br)ccc1CN1C(=O)c2cccn2[C@@]2(CC(=O)NC2=O)C1=O

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(-20℃)

With Ice Pack

≥ 2 years