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).
Sold for research purposes under agreement from GlaxoSmithKline
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 305.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.27 mL||16.37 mL||32.75 mL|
|5 mM||0.65 mL||3.27 mL||6.55 mL|
|10 mM||0.33 mL||1.64 mL||3.27 mL|
|50 mM||0.07 mL||0.33 mL||0.65 mL|
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for GSK 137647, please let us know.
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Keywords: GSK 137647, GSK 137647 supplier, GSK137647, Free, fatty, acid, receptor, 4, diabetes, potent, and, selective, FFA4, GPR120, agonist, Fatty, Acid, Receptors, 5257, Tocris Bioscience
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