Chemical Name: 4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide
Biological ActivityGSK 137647 is a potent and selective FFA4 (GPR120) agonist (pEC50 values are 6.3, 6.2 and 6.1 at the human, mouse and rat receptor, respectively). Exhibits ≥100-fold selectivity against a panel of 61 targets including FFA1, FFA2 and FFA3. Enhances glucose-stimulated insulin secretion in MIN6 cells. Induces intracellular calcium accumulation in U2OS cells; this activity is inhibited by AH 7614 (Cat. No. 5256).
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Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Sparks et al.
Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity.
Martin et al.
J.Lipid Res., 2012;53:2256
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