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CAS No.: 82159-09-9

依帕司他 Catalog No. CSN12976

Synonyms: ONO2235;Sorbistat;Epalrestatum

Epalrestat is an aldose reductase inhibitor with IC50 of 72 nM, and used for the treatment of diabetic neuropathy.

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生物活性

实验方案

技术信息

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]
动物研究
剂量
Rat: 100 mg/kg/day^[3] (p.o.), 13.5 mg/kg - 54 mg/kg^[4] (p.o.) Mice: 30 mg/kg - 300 mg/kg^[5] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Rat: 100 mg/kg/day^[3] (p.o.), 13.5 mg/kg - 54 mg/kg^[4] (p.o.) Mice: 30 mg/kg - 300 mg/kg^[5] (p.o.)
给药途径	p.o.

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 ... more >> 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 Collapse <<

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.

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
- 3.1309 mL
- 15.6544 mL
- 31.3087 mL
- 5 mM
- 0.6262 mL
- 3.1309 mL
- 6.2617 mL
- 10 mM
- 0.3131 mL
- 1.5654 mL
- 3.1309 mL

技术信息

CAS号

82159-09-9

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H13NO3S2

运输

蓝冰

分子量

319.40

别名

ONO2235;Sorbistat;Epalrestatum;Kinedak;依帕司他

溶解度

DMSO	3.0 mg/mL (9.4 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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