GSK137647A

Research use only, not for human use.

GSK137647A is a selective FFA4 agonist.

GSK137647A is an agonist of the free fatty acid receptor 4 (FFA4/GPR120) with pEC50s = 6.3, 6.2, and 6.1 at human, mouse, and rat receptors, respectively. GSK137647A is selective for GPR120 over a panel of 61 other targets, including other FFARs.

GSK137647A (GSK 137647) (50 μM) reduces the production of NO in macrophages without affecting cell viability.GSK137647A (GSK 137647) (30 μM; 12 hours) alleviates response to inflammatory stimuli in Caco-2 cells and induces secretion of IL-6.GSK137647A (GSK 137647) (10 μM) reduces the ion flow and affects the colonic epithelial ion transport in healthy. GSK137647A (GSK 137647) (50 μM) increases glucose stimulated insulin secretion. Western Blot Analysis Cell Line:Caco-2 cells Concentration:30 μM Incubation Time:12 hours Result:Down regulated FFAR1, FFAR2, and FFAR4 as compared to control.Cell Viability Assay Cell Line:RAW264.7 macrophages Concentration:10, 20 and 50 μM Incubation Time:24 hours Result:Without affected cell viability.

GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) alleviates colitis in TNBS- and DSS-treated mice.GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) restores intestinal permeability in vivo. Animal Model:Male C57BL/6 mice Dosage:1 mg/kg Administration:Intraperitoneal injection; twice daily, for 7 days Result:Had anti-inflammatory effect and reversed colonic injury induced by DSS.Animal Model:Male C57BL/6 mice Dosage:1 mg/kg Administration:Intraperitoneal injection; twice daily, for 7 days Result:Decreased the amount of FITC and alleviated intestinal epithelial barrier permeability.

GSK137647A | GSK-137647A

Endocrinology/Hormones

AChR

GPR120

Metabolic Disease

——

349085-82-1

305.39

C16H19NO3S

>98% (HPLC)

DMSO : ≥ 32 mg/mL. 104.78 mM; H2O : < 0.1 mg/mL

Cc1cc(c(c(c1)C)NS(=O)(=O)c1ccc(cc1)OC)C

4-methoxy-N-(2,4,6-trimethylphenyl)-benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years