Biological Activity
GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.IC50 value: 6.3/6.2/6.1 (pEC50, for human/mouse/rat FFA4)Target: FFA4The pEC50s for Human , Mouse and Rat FFA1/2/3 are ＜ 4.5. GSK137647A is evaluated against a panel of 65 targets in both full curve functional and binding assays and was shown to provide at least 100-fold selectivity against the panel which included 41 G-protein-coupled receptors (GPCRs), including additional members of the free fatty acid receptors (FFA1, FFA2, and FFA3). GSK137647A produces a concentration-dependent increase in glucose stimulated insulin secretion under high glucose conditions (25 mM).
In Vitro
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In Vivo
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References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.