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DC260126

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Chemical Structure| 346692-04-4 同义名 : -
CAS号 : 346692-04-4
货号 : A269842
分子式 : C16H18FNO2S
纯度 : 98%
分子量 : 307.383
MDL号 : MFCD00784423
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(341.59 mM)，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 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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.25mL

0.65mL

0.33mL

16.27mL

3.25mL

1.63mL

32.53mL

6.51mL

3.25mL
参考文献

[1]Wu J, Sun P, et al. Inhibition of GPR40 protects MIN6 β cells from palmitate-induced ER stress and apoptosis. J Cell Biochem. 2012 Apr;113(4):1152-8.

[2]Hu H, He LY, et al. A novel class of antagonists for the FFAs receptor GPR40. Biochem Biophys Res Commun. 2009 Dec 18;390(3):557-63.

[3]Sun P, Wang T, Zhou Y, Liu H, Jiang H, Zhu W, Wang H. DC260126: a small-molecule antagonist of GPR40 that protects against pancreatic β-Cells dysfunction in db/db mice. PLoS One. 2013 Jun 11;8(6):e66744