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Ranirestat

    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 147254-64-6
  • 分子式: C17H11BrFN3O4
  • 分子量: 420.19
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
R656799-1ml
1ml 期货 Stock Image

基本描述

别名 雷尼司他
规格或纯度 10mM in DMSO
英文名称 Ranirestat
生化机理 雷尼司他(AS-3201)是一种有效的口服活性醛糖还原酶(AR)抑制剂,对大鼠晶状体 AR 和重组人 AR 的 IC 50 s 分别为 11 nM 和 15 nM,对重组人 AR 的 K i 为 0.38 nM。雷尼司他具有治疗糖尿病的潜力。
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍


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 retinas

In Vitro

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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 . 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)

关联靶点(人)

AKR1B1 Tclin 醛糖还原酶(Aldose reductase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Isomeric SMILES C1C(=O)NC(=O)[C@@]12C(=O)N(C(=O)C3=CC=CN23)CC4=C(C=C(C=C4)Br)F
关联CAS 147254-64-6
PubChem CID 153948
MeSH Entry Terms 2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo(1,2-a)pyrazine-4-spiro-3'-pyrrolidine-1.2',3,5'-tetrone;AS 3201;AS-3201;ranirestat;SX 3030;SX 3202;SX-3030;SX-3202
分子量 420.19

安全和危险性(GHS)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
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