GSK137647A|GSK-137647A|FFA4 (GPR120) agonist

Cas No.:	349085-82-1
Chemical Name:	4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide
Synonyms:	GSK137647A,GSK 137647A,GSK-137647A
SMILES:	CC1=CC(C)=C(NS(C2=CC=C(OC)C=C2)(=O)=O)C(C)=C1
Formula:	C₁₆H₁₉NO₃S
M.Wt:	305.39
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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).

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC9981	TUG891	TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively.
DC5073	TAK-875(Fasiglifam)	TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 μM.
DC8577	FFA4 (GPR120) agonist GSK137647A	GSK-137647 is a potent and selective FFA4 (GPR120) agonist (pEC50 values are 6.3, 6.2 and 6.1 at the human, mouse and rat receptor, respectively). Exhibits ≥100-fold selectivity against a panel of 61 targets including FFA1, FFA2 and FFA3.
DC8593	GPR120 Compound A	GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µm) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).
DC10554	DC260126	DC260126, a small-molecule antagonist of GPR40.
DC7867	AMG-837	AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

FFA4 (GPR120) agonist GSK137647A