1. GPCR/G Protein
  2. 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 (11):

Cat. No. Product Name Effect Purity
  • HY-10480
    TAK-875 Activator 98.77%
    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. GW1100 acts as a GPR40 inverse agonist.
  • 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-15697
    TUG-770 Agonist 98.94%
    TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.
  • 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-103083
    FAA1 agonist-1 Agonist 98.97%
    FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
  • HY-101906
    DC260126 Antagonist 99.70%
    DC260126, a small-molecule antagonist of GPR40.
  • 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-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-13971
    GPR40 Activator 1 Activator
    GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.