产品说明书

	同义名 :	TAK-875 hemihydrate;Fasiglifam(TAK-875) Hemihydrate
	CAS号 :	1374598-80-7
	货号 :	A763280
	分子式 :	C58H66O15S2
	纯度 :	98+%
	分子量 :	1067.266
	MDL号 :	MFCD28010046
	存储条件：	粉末 液体 -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
描述	TAK-875 is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.

细胞研究
细胞系	浓度	检测类型	检测时间	活动说明	数据源
CHO cells		Function assay		Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA, EC50=0.016 μM	22490067
human 1321N1 cells		Function assay		Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry, EC50=14.13 nM	21854074

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	0.94mL 0.19mL 0.09mL	4.68mL 0.94mL 0.47mL	9.37mL 1.87mL 0.94mL

参考文献

[1]Kaku K, Enya K, et al. Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial. Diabetes Obes Metab. 2015 Jul;17(7):675-81. [2]Tsujihata Y, Ito R, et al. TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J Pharmacol Exp Ther. 2011 Oct;339(1):228-37.