A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM.

A potent, orally bioavailable, full agonist of GPR40/FFA1 with EC50 of 0.16 uM.

A potent, selective, orally available GPR40 agonist with EC50 of 8 nM.

A potent, selective, orally available GPR40 agonist with EC50 of 9 nM.

A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM.

A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays.

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.

DC260126, a small-molecule antagonist of GPR40.

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).

GPR40 AgoPAM AP5 is a potent, selective GPR40 AgoPAM (full agonist with positive allosteric modulation) with hIP1 EC50 of 0.8 nM, high selectivity over the GPR120 receptor (EC50>30 uM).

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.

GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99.

LY2922470 (LY-2922470) is a potent, selective, orally available GPR40 agonist with EC50 of 7 nM.

PBI-4050 (Setogepram, PBI4050) is a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, respectively.

PBI-4050 (Setogepram, PBI4050) is a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, respectively.

TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 μM.

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.

FFA2R agonist 58 is a potent, allosteric FFAR2 (GPR43) agonist/modulator.FFA2R agonist 58 functions as a positive/priming modulator in these cells by turning the natural FFA2R agonist acetate into a potent activator of the neutrophil NADPH-oxidase.FFA2R agonist 58 lowers the concentration of acetate required to induce a transient rise in the concentration of intracellular Ca2+ in neutrophils, has no direct effect on the neutrophil NADPH-oxidase activity but affects the response induced by acetate.FFA2R agonist 58 significantly reduced the amount of internalized influenza A virus (IAV) in treated A549 cells.

MK-8666 is a selective partial GPR40 agonist developed for the treatment of type 2 diabetes mellitus.

Xelaglifam is a potent GPR40 agonist. Antihyperglycaemic activity.

BI-2081 is a GPR40 (FFAR1) partial agonist (EC50: 4 nM). BI-2081 induces glucose depending insulin secretion and reduces the plasma glucose concentration. BI-2081 can be used in the research of metabolic diseases, in particular diabetes type 2.

TP-051 is a potent FFAR1 agonist with an Ki value of 16 nM for human FFAR1. TP-051 can increase insulin secretion in rat insulinoma cells. TP-051 can be used to research type 2 diabetes.