Cat. No. 5257
Chemical Name: 4-Methoxy-N-(2,4,6-trimethylphenyl)
Biological ActivityPotent 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).
Licensing InformationSold for research purposes under agreement from GlaxoSmithKline
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Sparks et al (2014) Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg.Med.Chem.Lett. 24 3100. PMID: 24881566.
Martin et al (2012) Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity. J.Lipid Res. 53 2256. PMID: 22904345.
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Keywords: GSK 137647, supplier, GSK137647, Free, fatty, acid, receptor, 4, diabetes, potent, and, selective, FFA4, GPR120, agonist, Tocris Bioscience, Free Fatty Acid Receptor Agonist products
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