GSK 137647
Discontinued Product
Chemical Name: 4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide
Purity: ≥99%
Biological Activity
GSK 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).Technical Data
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.
Additional Information
Background References
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Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Sparks et al.
Bioorg.Med.Chem.Lett., 2014;24:3100 -
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 -
Secreted Phospholipase PLA2G2D Contributes to Metabolic Health by Mobilizing ?3 Polyunsaturated Fatty Acids in WAT
H Sato, Y Taketomi, Y Miki, R Murase, K Yamamoto, M Murakami
Cell Rep, 2020;31(5):107579.
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