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Epalrestat

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Chemical Structure| 82159-09-9 同义名 : 依帕斯他 ;ONO2235
CAS号 : 82159-09-9
货号 : A245255
分子式 : C15H13NO3S2
纯度 : 95%
分子量 : 319.4
MDL号 : -
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(56.36 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
动物实验配方：
生物活性
描述 Aldose reductase, a cytosolic oxidoreductase in the polyol pathway that catalyzes the reduction of a variety of aldehydes and carbonyls, including the reduction of glucose to sorbitol, is important for various organs. Epalrestat is a noncompetitive and reversible aldose reductase inhibitor with IC50 of 72 nM. Epalrestat can reduce sorbitol accumulation both in animals and in humans by attenuating high glucose-mediated neutrophil-endothelial cell adhesion and decreasing the levels of carboxymethyl-lysine. 50 mg oral administration of epalrestat could reach a peak plasma concentration of 3.9 µg/ml only in 1 hr in healthy adults with a protein binding rate of 90.1%. In patients with somatic diabetic neuropathy, the treatment group received epalrestat 50 mg 3 times/day had a significant increase from baseline in MNCV and SNCV as well as the significant difference from baseline in the threshold of vibratory sensation and the higher disappearance rate of spontaneous pain in the upper limbs and lower limbs. In another group, 45 non–insulin-dependent diabetes patients also received 50 mg epalrestat 3 times/day, the results reported significant improvement regarding spontaneous pain, not significant upper extremities and significant VPT in right tibial and radial styloid processes. 28 patients with mild or no symptoms of diabetic neuropathy were treated with 150 mg/day epalrestat, the least F wave latencies and tibial motor nerves were not shortened[1] . In mice plasma, the linearity with a correlation coefficient of 0.9994 was obtained when examined by epalrestat with range of 2-5000 ng/ml and the accuracy and precision were significant in a dose-dependent way with average RSD% values less than 12.3%. Epalrestat could be rapidly absorbed and distributed in many tissues at 10 min after oral administration.[2]
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03244358 Triple Negative Breast Cancer Phase 2 Recruiting July 1, 2018 China, Guangdong ... 展开 >> Sun Yat-sen University, Cancer Center Recruiting Guangzhou, Guangdong, China, 510060 Contact: Yuan Zhong-yu, MD    86-20-87342496    yuanzhy@sysucc.org.cn    Contact: Huang Jia-Jia, MD    86-20-87343794    huangjiaj@sysucc.org.cn    Principal Investigator: Yuan Zhong-yu, MD          Sub-Investigator: Huang Jia-Jia, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.13mL

0.63mL

0.31mL

15.65mL

3.13mL

1.57mL

31.31mL

6.26mL

3.13mL
参考文献

[1]Ramirez MA, Borja NL. Epalrestat: an aldose reductase inhibitor for the treatment of diabetic neuropathy. Pharmacotherapy. 2008 May;28(5):646-55.

[2]Teng W, Li W, et al. Identification of quantitative trait loci underlying seed protein content of soybean including main, epistatic, and QTL × environment effects in different regions of Northeast China. Genome. 2017;60(8):649-655.