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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. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.92mL 0.78mL 0.39mL |
19.59mL 3.92mL 1.96mL |
39.18mL 7.84mL 3.92mL |
CAS号 | 51411-04-2 |
分子式 | C14H9NO4 |
分子量 | 255.226 |
别名 | AY-22284;NSC 299132 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 50 mg/mL(195.91 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |