GSK137647A_product_DataBase

Bioactivity

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].

Invitro

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]. Western Blot Analysis[1] Cell Line:

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]. Animal Model:

Name

GSK137647A

CAS

349085-82-1

Formula

C16H19NO3S

Molar Mass

305.39

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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. [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.

PeptideDB

GSK137647A

CAS: 349085-82-1 F: C16H19NO3S W: 305.39