|DC260126游离态|CsnPharm

CAS No.: 346692-04-4

DC260126 is antagoniat of free fatty acid receptor 1 (FFA1/GPR40) and inhibits FFA-induced the increase of intracellular Ca2+ level.

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400-920-2911

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400-920-2911

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描述The G-protein coupled receptor 40 (GPR40) mediates both acute and chronic effects of FFAs (free fatty acid) on insulin secretion and plays an important role in glucose homeostasis. DC260126 is a small-molecule GPR40 antagonist. In db/db mice, the FSI (fasting serum insulin) level was decreased dose-dependently after giving different dose of DC260126 for 5 days. Both 10 and 30 mg/kg DC260126 could reduce FSI level of db/db mice significantly. Further, DC260126 could lower fasted serum insulin levels and alter glucose-stimulated insulin secretion in db/db mice. In DC260126 treated db/db mice, insulin expression was decreased in islet compared with vehicle treated mice. Moreover, DC260126-treated mice showed an obvious decrease of blood glucose levels during ITT in response to insulin compared to the vehicle-treated group. Lastly, the phase 2 of glucose-stimulated insulin secretion was obviously suppressed in DC260126-treated db/db mice in comparison with vehicle group^[3]. Also, DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis Wu J, Sun P, Zhang X, Liu H, Jiang H, Zhu W, Wang H. Inhibition of GPR40 protects MIN6 β cells from palmitate-induced ER stress and apoptosis. J Cell Biochem. 2012 Apr;113(4):1152-8. doi: 10.1002/jcb.23450. Erratum in: J Cell Biochem. 2013 May;114(5):1216.
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实验方案

技术信息

CAS号

346692-04-4

储存条件

分子式

C16H18FNO2S

运输

蓝冰

分子量

307.38

别名

溶解度

DMSO	100.0 mg/mL (325.3 mM)

动物实验配方

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