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产品总数：60950
| 中文名称 |
Ranirestat
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|---|---|
| 中文别名 |
雷尼司他;Ranirestat
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| 英文名称 |
Ranirestat
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| 英文别名 |
Spiro[pyrrolidine-3,4'(1'H)-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetrone,2'-[(4-bromo-2-fluorophenyl)methyl]-, (3R)-;(3R)-2'-[(4-bromo-2-fluorophenyl)methyl]spiro[pyrrolidine-3,4'-pyrrolo[1,2-a]pyrazine]-1',2,3',5-tetrone;AS-3201;Spiro[pyrrolidine-3,4'(1'H)-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetrone,2'-[(4-bromo-2-fluo...;(3R)-2'-(4-bromo-2-fluorobenzyl)spiro[pyrrolidin-3,4'(1'H)-pyrrolo[1,2-a]pyrazin]-1',2,3',5(2'H)-tetraone;(3R)-2'-(4-bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'(1'H)-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2H')-tetraone;(R)-2-(4-bromo-2-fluorobenzyl)spiro[1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4,3'-pyrrolidine]-1,2',3,5'-tetrone;AC1L4BEU;CHEMBL334830;R-(-)-2-(4-bromo-2-fluoroben;SX 3030;SX-3030;SX-3202;(3R)-2′-[(4-Bromo-2-fluorophenyl)methyl]-spiro[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2′H)-tetrone.;(3R)-2'-(4-Bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'-1'H-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetraone;AS 3201;Raniestat;Ranirestat;Ranirestat,AS-3201;Spiro[pyrrolidine-3,4'(1'H)-pyrrolo[1,2-a]pyrazine]-1',2,3',5(2'H)-tetrone,2'-[(4-broMo-2-fluorophenyl)Methyl]-, (3R)-
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| Cas No. |
147254-64-6
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| 分子式 |
C17H11N3O4FBr
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| 分子量 |
420.19
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| 包装储存 |
Powder -20°C 3 years；4°C 2 years
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| 产品详情 |
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。
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|---|---|
| 生物活性 |
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.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
IC50: 11 nM (Rat lens aldose reductase) and 15 nM (Recombinant humanaldose reductase)
Ki: 0.38 nM (Recombinant humanaldose reductase)
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| 体外研究(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 IC50 values of 0.010 μM and 0.041 μM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years；4°C 2 years
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| ClinicalTrial |
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| 参考文献 |
[1]. 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.[2]. 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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| 溶解度数据 |
In Vitro: DMSO : ≥ 50 mg/mL (118.99 mM)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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