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CAS No.: 51411-04-2

Alrestatin Catalog No. CSN10270

Synonyms: AY-22284;NSC 299132

Alrestatin is an inhibitor of aldose reductase, an enzyme involved in the pathogenesis of complications of diabetes mellitus, including diabetic neuropathy.

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生物活性

描述Aldose reductase is a monomeric, cytosolic enzyme that catalyzes the NADPH-dependent reduction of carbonyl compounds. Alrestatin is an aldose reductase inhibitor that inhibits the wild type aldose reductase, R311A mutant and R308A mutant with IC₅₀ values of 148, 119, and 67.3 µM^[3]. In rat vascular smooth muscle cells, alrestatin at 10 μM minimized high glucose-induced accumulation of Angiotensin II in cells and media, and attenuated the decrease in Angiotensin I level in media^[4]. The intraperitoneal administration of alrestatin in rats immediately after pyloric ligation inhibited gastric acid secretion with an ED₅₀ value of 90 mg/kg. The oral administration of alrestatin 1 h before pyloric ligation also inhibited gastric acid secretion with an ED₅₀ of 180 mg/kg. Alrestatin induced ulcer formation in rats with an ED₅₀ of 330 mg/kg via intraperitoneal administration^[5].
作用机制Alrestatin is an orally active aldose reductase inhibitor that binds preferentially to the enzyme/NADP⁺ complex. The mutation of the Trp20 residue (W20A) greatly affected the binding of alrestatin and enzyme inhibition.
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9181 mL
- 19.5905 mL
- 39.1810 mL
- 5 mM
- 0.7836 mL
- 3.9181 mL
- 7.8362 mL
- 10 mM
- 0.3918 mL
- 1.9591 mL
- 3.9181 mL

技术信息

CAS号

51411-04-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H9NO4

运输

蓝冰

分子量

255.23

别名

AY-22284;NSC 299132

溶解度

DMSO	60.0 mg/mL (235.1 mM)
Water	insoluble

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