MedChemExpress - Model GSK137647A - 349085-82-1

FromMedChemExpress LLC (MCE)

GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response[1][2].

GSK137647A

MCE China：GSK137647A

Brand：MedChemExpress (MCE)

Cat. No.HY-19995

CAS：349085-82-1

Synonyms：GSK 137647

Purity：99.81%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response.

In Vitro：GSK137647A (GSK 137647) (50 μM) reduces the production of NO in macrophages without affecting cell viability[1]. GSK137647A (GSK 137647) (30 μM; 12 hours) alleviates response to inflammatory stimuli in Caco-2 cells and induces secretion of IL-6[1]. GSK137647A (GSK 137647) (10 μM) reduces the ion flow and affects the colonic epithelial ion transport in healthy[1]. GSK137647A (GSK 137647) (50 μM) increases glucose stimulated insulin secretion[2].

In Vivo：GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) alleviates colitis in TNBS- and DSS-treated mice[1]. GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) restores intestinal permeability in vivo[1].

References：

[1]. Salaga M, et, al. Activation of Free Fatty Acid Receptor 4 Affects Intestinal Inflammation and Improves Colon Permeability in Mice. Nutrients. 2021 Aug 6;13(8):2716. [Content Brief]

[2]. Sparks SM, et, al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3. [Content Brief]

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