1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR40

GPR40

GPR40 (Free fatty acid receptor 1, FFA1) is a class A G-protein coupled receptor that in humans is encoded by the FFAR1 gene. It is strongly expressed in the cells of the pancreas and to a lesser extent in the brain. This membrane protein binds free fatty acids, acting as a nutrient sensor for regulating energy homeostasis. GPR40 is activated by medium to long chain fatty acids. GPR40 is most strongly activated by eicosatrienoic acid, but has been found to be activated by fatty acids as small as 10 carbons long. For saturated fatty acids the level of activation is dependent on the length of the carbon chain, which is not true for unsaturated fatty acids. It has been found that three hydrophilic residues (arginine-183, asparagine-244, and arginine-258) anchor the carboxylate group of a fatty acid, which activates GPR40.

GPR40 Related Products (22):

Cat. No. Product Name Effect Purity
  • HY-10480
    Fasiglifam Activator 98.94%
    Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.
  • HY-50691
    GW-1100 Antagonist
    GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.
  • HY-100775
    Setogepram sodium salt Agonist 99.65%
    Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Setogepram sodium salt decreases renal, liver and pancreatic fibrosis. Setogepram sodium salt exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
  • HY-15589
    GW9508 Agonist 99.19%
    GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.
  • HY-13967B
    AMG 837 calcium hydrate Agonist 98.01%
    AMG 837 calcium hydrate is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
  • HY-100775A
    Setogepram Agonist
    Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
  • HY-130120
    HWL-088 Agonist
    HWL-088 (compound 7) is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist bearing a phenoxyacetic acid scaffold. HWL-088 significantly improves glucose tolerance in normal and diabetic models.
  • HY-14363
    TUG-424 Agonist >98.0%
    TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity.
  • HY-101906
    DC260126 Antagonist 99.70%
    DC260126, a small-molecule antagonist of GPR40.
  • HY-13467
    AM-1638 Agonist 99.42%
    AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
  • HY-15697
    TUG-770 Agonist 98.52%
    TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.
  • HY-12647
    GPR40 Activator 2 Activator 99.63%
    GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
  • HY-19835
    LY2922470 Agonist 99.87%
    LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM).
  • HY-103083
    GPR40 agonist 4 Agonist 98.97%
    GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
  • HY-13967
    AMG 837 Agonist
    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.
  • HY-13967A
    AMG 837 sodium salt Agonist
    AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
  • HY-12585
    AM-4668 Agonist >99.0%
    AM-4668 is a GPR40 agonist for type 2 diabetes. EC50s of 3.6 nM and 36 nM for GPR40 in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), respectively.
  • HY-111359
    GPR40 agonist 1 Agonist
    GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
  • HY-112603
    AP5 Agonist
    AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor.
  • HY-111763
    GPR40/FFAR1 modulator 1 Agonist
    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
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