349085-82-1

349085-82-1 structure

Name: GSK137647A
Chemical Name: 4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide
CAS Number: 349085-82-1
Molecular Formula: C₁₆H₁₉NO₃S
Molecular Weight: 305.39200
Catalog: Signaling Pathways GPCR/G Protein GPR120
Create Date: 2019-03-29 21:15:17
Modify Date: 2024-01-03 11:25:26
GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.IC50 value: 6.3/6.2/6.1 (pEC50, for human/mouse/rat FFA4)Target: FFA4The pEC50s for Human , Mouse and Rat FFA1/2/3 are ＜ 4.5. GSK137647A is evaluated against a panel of 65 targets in both full curve functional and binding assays and was shown to provide at least 100-fold selectivity against the panel which included 41 G-protein-coupled receptors (GPCRs), including additional members of the free fatty acid receptors (FFA1, FFA2, and FFA3). GSK137647A produces a concentration-dependent increase in glucose stimulated insulin secretion under high glucose conditions (25 mM).

Name	4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide
Synonyms	gsk 137647 GSK137647A

Description	GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.IC50 value: 6.3/6.2/6.1 (pEC50, for human/mouse/rat FFA4)Target: FFA4The pEC50s for Human , Mouse and Rat FFA1/2/3 are ＜ 4.5. GSK137647A is evaluated against a panel of 65 targets in both full curve functional and binding assays and was shown to provide at least 100-fold selectivity against the panel which included 41 G-protein-coupled receptors (GPCRs), including additional members of the free fatty acid receptors (FFA1, FFA2, and FFA3). GSK137647A produces a concentration-dependent increase in glucose stimulated insulin secretion under high glucose conditions (25 mM).
Related Catalog	Signaling Pathways >> GPCR/G Protein >> GPR120 Research Areas >> Metabolic Disease
References	[1]. 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.

RIDADR	NONH for all modes of transport