货号 | 17712-5mg |
描述 | 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.1,2 GSK137647A is a diarylsulfonamide that acts as a selective agonist of GPR120 (pEC50s = 6.3, 6.2, and 6.1 at human, mouse, and rat receptors, respectively).3,4 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.4 It also modestly stimulates the production of glucagon-like peptide-1 in taste bud cells and human intestinal NCI-H716 cells.3,4 |
供应商 | Cayman |
应用文献 | |
1.Davenport, A.P.,Alexander, S.P.H.,Sharman, J.L., et al. International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: Recommendations for new pairings with cognate ligands. Pharmacological Reviews 65(3), 967-986 (2013). 2.Oh, D.Y.,Talukdar, S.,Bae, E.J., et al. GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin sensitizing effects. Cell 142(5), 687-698 (2010). 3.Martin, C.,Passilly-Degrace, P.,Chevrot, M., et al. Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: Putative involvement of GPR120 and impact on taste sensitivity. Journal of Lipid Research 53(11), 2256-2265 (2012). 4.Sparks, S.M.,Chen, G.,Collins, J.L., et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorganic & Medicinal Chemistry Letters 24, 3100-3103 (2014). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 305.4 |
分子式 | C16H19NO3S |
CAS号 | 349085-82-1 |
稳定性 | ≥ 2 years |
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