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Home >> Signaling Pathways >> GPCR/G protein >> FFAR1 (GPR40)

FFAR1 (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.

Products for  FFAR1 (GPR40)

  1. Cat.No. Product Name Information
  2. GC31607 AM-1638 AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM. AM-1638 Chemical Structure
  3. GC34464 AM-4668 AM-4668 is a GPR40 agonist for type 2 diabetes. AM-4668 Chemical Structure
  4. GC19030 AMG 837 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 AMG 837 Chemical Structure
  5. GC35313 AMG 837 calcium hydrate AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate Chemical Structure
  6. GC35314 AMG 837 sodium salt 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. AMG 837 sodium salt Chemical Structure
  7. GC35364 AP5 AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 Chemical Structure
  8. GC18125 DC260126 free fatty acid receptor 1 (FFAR1/GPR40) antagonist DC260126 Chemical Structure
  9. GC31410 FAA1 agonist-1 FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54. FAA1 agonist-1 Chemical Structure
  10. GC36185 GPR40 Activator 1 GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes. GPR40 Activator 1 Chemical Structure
  11. GC31389 GPR40 Activator 2 GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1. GPR40 Activator 2 Chemical Structure
  12. GC31634 GPR40 Agonist 2 GPR40 Agonist 2 is a GPR40 agonist that can be used in the research of diabetes, extracted from patent WO2009054479A1. GPR40 Agonist 2 Chemical Structure
  13. GC14027 GW-1100 A selective GPR40 antagonist GW-1100 Chemical Structure
  14. GC12401 GW9508 FFA1/GPR40 agonist,potent and selective GW9508 Chemical Structure
  15. GC63010 HWL-088 HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 Chemical Structure
  16. GC36507 LY2922470 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 Chemical Structure
  17. GC31698 PBI-4050 sodium salt (Setogepram (sodium salt)) Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. PBI-4050 sodium salt (Setogepram (sodium salt)) Chemical Structure
  18. GC16555 TAK-875 TAK-875 (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM. TAK-875 Chemical Structure
  19. GC10922 TUG 424 FFA1 (GPR40) agonist TUG 424 Chemical Structure
  20. GC16054 TUG-770 An agonist of FFA1/GPR40 TUG-770 Chemical Structure
  21. GC32481 Vincamine A plant alkaloid with vasodilator effects Vincamine Chemical Structure

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