Lidorestat|245116-90-9|(IDD-676)-陌孚医药/Medlife

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Lidorestat (Synonyms: IDD-676)

目录号: PL01551 纯度: ≥99%

CAS No. :245116-90-9

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中文名称	Lidorestat
中文别名	利多司他
英文名称	Lidorestat
英文别名	1H-Indole-1-aceticacid, 3-[(4,5,7-trifluoro-2-benzothiazolyl)methyl]-;LIDORESTAT;2-[3-[(4,5,7-trifluoro-1,3-benzothiazol-2-yl)methyl]indol-1-yl]acetic acid;{3-[(4,5,7-trifluoro-1,3-benzothiazol-2-yl)methyl]-1H-indol-1-yl}acetic acid;EML-676;IDD-000676-01;IDD-676;[3-(4,5,7-Trifluorobenzothiazol-2-ylmethyl)indol-1-yl]acetic acid;3-[(4,5,7-Trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid
Cas No.	245116-90-9
分子式	C₁₈H₁₁N₂O₂F₃S
分子量	376.35
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Lidorestat (IDD-676) 是一种有效的，选择性的，口服活性的醛糖还原酶 (aldose reductase) 抑制剂，IC₅₀ 为 5 nM。Lidorestat 可用于慢性糖尿病并发症。Lidorestat 还可改善神经传导并减少白内障形成。

生物活性

Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC 50 of 5 nM. Lidorestat can be used for chronic diabetes complications. Lidorestat also improves nerve conduction and reduces cataract formation.

性状

Solid

IC50 & Target[1][2]

IC50: 5 nM (Rldose reductase)

体外研究(In Vitro)

From in vitro experiments, Lidorestat has a reported IC50 against recombinant human aldose reductase (/h/-ALR2) of 5 μM. Against recombinant human aldehyde reductase (/h/-ALR1), Lidorestat has a reported IC50 of 27,000 μM, yielding a selectivity of /h/-ALR1//h/-ALR2 of 5400:1. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Lidorestat (25 mg/kg/day; oral administration; twice daily; for 6 weeks; diabetic mice) treatment decreases fructose and reduces mortality in diabetic hAR-expressing mice. And Lidorestat does not affect weight. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Noh HL, et al. Regulation of plasma fructose and mortality in mice by the aldose reductase inhibitor lidorestat. J Pharmacol Exp Ther. 2009 Feb;328(2):496-503.
[2]. Van Zandt MC, et al. Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. J Med Chem. 2005 M

溶解度数据	In Vitro: DMSO : 50 mg/mL (132.86 mM; ultrasonic and warming and heat to 60°C)配制储备液

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产品使用指南

Data Sheet

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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