GSK137647A

GPR120 (Free Fatty Acid Receptor 4, FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. GSK137647A is a diarylsulfonamide that acts as a selective agonist of GPR120 (EC50s = 0.5, 0.63, and 0.79 µM for human, mouse, and rat receptors, respectively). It is selective for GPR120 over a panel of 61 other targets, including other FFARs. Like the natural GPR120 ligand linoleic acid, GSK137647A dose-dependently stimulates insulin secretion by mouse insulinoma MIN6 cells under high glucose conditions. It also modestly stimulates the production of glucagon-like peptide-1 in taste bud cells and human intestinal NCI-H716 cells.Formal Name: 4-methoxy-N-(2,4,6-trimethylphenyl)-benzenesulfonamide. CAS Number: 349085-82-1. Molecular Formula: C16H19NO3S. Formula Weight: 305.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml, Ethanol: 1 mg/ml. lambdamax: 242 nm. SMILES: COC1=CC=C(S(NC2=C(C)C=C(C)C=C2C)(=O)=O)C=C1. InChi Code: InChI=1S/C16H19NO3S/c1-11-9-12(2)16(13(3)10-11)17-21(18,19)15-7-5-14(20-4)6-8-15/h5-10,17H,1-4H3. InChi Key: FQUAFMNPXPXOJE-UHFFFAOYSA-N.