| DC11994 |
ZQ-16 |
A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM. |
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| DC11697 |
AM-1638 |
A potent, orally bioavailable, full agonist of GPR40/FFA1 with EC50 of 0.16 uM. |
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| DC11683 |
LY2881835 |
A potent, selective, orally available GPR40 agonist with EC50 of 8 nM. |
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| DC11682 |
LY2922083 |
A potent, selective, orally available GPR40 agonist with EC50 of 9 nM. |
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| DC11680 |
LY3104607 |
A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM. |
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| DC11623 |
GPR120 agonist 4x |
A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays. |
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| DC7867 |
AMG-837
Featured
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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. |
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| DC10554 |
DC260126
Featured
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DC260126, a small-molecule antagonist of GPR40. |
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| DC8593 |
GPR120 Compound A
Featured
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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). |
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| DC11143 |
GPR40 AgoPAM AP5 |
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). |
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| DC8577 |
FFA4 (GPR120) agonist GSK137647A
Featured
|
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. |
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| DC9458 |
GW-1100 |
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.
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| DC11681 |
LY2922470 |
LY2922470 (LY-2922470) is a potent, selective, orally available GPR40 agonist with EC50 of 7 nM. |
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| DC11100 |
PBI-4050 sodium |
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. |
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| DC11099 |
PBI-4050 |
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. |
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| DC5073 |
TAK-875(Fasiglifam)
Featured
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TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 μM. |
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| DC9981 |
TUG891
Featured
|
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. |
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| DC70406 |
FFAR2 agonist 58 |
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. |
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| DC70601 |
MK-8666 |
MK-8666 is a selective partial GPR40 agonist developed for the treatment of type 2 diabetes mellitus. |
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| DC71955 |
Xelaglifam |
Xelaglifam is a potent GPR40 agonist. Antihyperglycaemic activity. |
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| DC72259 |
BI-2081 |
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. |
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| DC72260 |
TP-051 |
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. |
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| DC72534 |
TUG-469 |
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. |
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| DC72535 |
TUG-499
Featured
|
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. |
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| DC73432 |
2CTAP |
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. |
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| DC73433 |
AZ13595491 |
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. |
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| DC73434 |
AZ423 |
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. |
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| DC73435 |
CPL207280 |
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). |
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| DC73436 |
MK-2305 |
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). |
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| DC73437 |
Phenylacetamide 2 |
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. |
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