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.

TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes.

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes.

2CTAP is a small molecule inverse agonist of FFA2 receptor signalling, inhibits constitutive Ca2+ levels, antagonised acetate-induced pERK1/2 and prevents damage following IRI, has no effect on cAMP.

AZ13595491 (AZ491) is a potent, selective G-protein-coupled receptor GPR120 (FFAR4) agonist with IC50 of 0.74/1.0 uM for huamn/mouse GPR120, respectively.

AZ423 (AZ13595423, AZ-423) is a potent, selective G-protein-coupled receptor GPR120 (FFAR4) agonist with IC50 of 0.36/0.51 uM for huamn/mouse GPR120, respectively.

CPL207280 (CPL 207280) is a novel potent, selective GPR40/FFA1 agonist with EC50 of 80 nM in a Ca2+ influx assay, shows greater potency than fasiglifam (EC50=270 nM).

MK-2305 (MK2305) is a potent and selective partial GPR40 (FFAR1) agonist with EC50 of 6 nM (rat GPR40), stimulates glucose stimulated insulin secretion (GSIS).

Phenylacetamide 2 (FFA2 allosteric agonist 2) is a potent, specific and allosteric agonist of FFA2 (GPR43) with cAMP IC50 of 0.48 and 0.66 uM for hFFA2 and mFFA2, respectively.

TUG-2304 (TUG2304) is a highly potent FFA2 (GPR43) antagonist with IC50 of 3-4 nM in both cAMP and GTPγS assays.