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- TAK875 1000413-72-8

- TAK875 1000413-72-8
TAK875 1000413-72-8
产品描述 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.
纯度 >98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 TAK-875;Fasiglifam外观 White to off white solid可溶性/溶解性 DMSO : ≥ 128 mg/mL (243.98 mM)生物活性 靶点 GPR40In vitro(体外研究) TAK-875 (0.01-10 μM) produces a concentration-dependent increase in intracellular IP production in CHO-hGPR40, with EC50 of 0.072 μM. TAK-875 (0.1-10 μM) dose-dependently augments intracellular IP production in CHO cells. TAK-875 (3-30 μM) concentration-dependently augments i. In the presence of 10 mM glucose, TAK-875 (0.001-10 μM) dose-dependently stimulats insulin secretion from INS-1 833/15 cells.In vivo(体内研究) TAK-875 (10 mg/kg, p.o.) increases plasma insulin levels in ZDF rats. TAK-875 (30 mg/kg, p.o.) improves fasting hyperglycemia without affecting fasting normoglycemia. TAK-875 at 30 mg/kg, which is a 3- to 10-fold higher dose compared with the dose that improved glucose tolerance in diabetic rats, does not alter fasting glucose levels in SD rats with normal glucose homeostasis. Likewise, TAK-875 does not significantly alter insulin secretion in SD rats with normal fasting glucose levels .参考文献 参考文献 研究领域 研究领域 Drug DiscoverySmall Molecule DrugLead Compound DiscoveryTAK875 1000413-72-8温馨提示:本产品仅作科研实验使用,不支持临床等研究
