FFAR1 (GPR40)
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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 Related to FFAR1 (GPR40)(20)
- GC31389GPR40 Activator 2CAS: 1312787-30-6Purity: >99.50%
GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
- GC31410FAA1 agonist-1CAS: 2102196-57-4Purity: >98.50%
FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
- GC31634GPR40 Agonist 2CAS: 1147729-48-3Purity: >98%
GPR40 Agonist 2 is a GPR40 agonist that can be used in the research of diabetes, extracted from patent WO2009054479A1.
- GC31698PBI-4050 sodium salt (Setogepram (sodium salt))CAS: 1254472-97-3Purity: >99.50%
Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84.
- GC35313AMG 837 calcium hydrateCAS: 1259389-38-2Purity: >98%
AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1.
- GC35314AMG 837 sodium saltCAS: 865231-45-4Purity: >98%
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.
- GC36185GPR40 Activator 1CAS: 1309435-60-6Purity: >98.50%
GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC10922 | TUG 424 | 1082058-99-8 | >98.00% | |
FFA1 (GPR40) agonist | ||||
| GC12401 | GW9508 | 885101-89-3 | >98.00% | |
FFA1/GPR40 agonist,potent and selective | ||||
| GC14027 | GW-1100 | 306974-70-9 | >98% | |
A selective GPR40 antagonist | ||||
| GC16054 | TUG-770 | 1402601-82-4 | >99.50% | |
An agonist of FFA1/GPR40 | ||||
| GC16555 | TAK-875 | 1000413-72-8 | >98.50% | |
TAK-875 is a potent, selective and orally bioavailable GPR40 (G protein-coupled receptor 40) agonist with an EC 50 value of 0.014μM for human GPR40. | ||||
| GC18125 | DC260126 | 346692-04-4 | >98.00% | |
free fatty acid receptor 1 (FFAR1/GPR40) antagonist | ||||
| GC19030 | AMG 837 | 865231-46-5 | >98% | |
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 | ||||
| GC31389 | GPR40 Activator 2 | 1312787-30-6 | >99.50% | |
GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1. | ||||
| GC31410 | FAA1 agonist-1 | 2102196-57-4 | >98.50% | |
FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54. | ||||
| GC31607 | AM-1638 | 1142214-62-7 | >99.50% | |
AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM. | ||||
| GC31634 | GPR40 Agonist 2 | 1147729-48-3 | >98% | |
GPR40 Agonist 2 is a GPR40 agonist that can be used in the research of diabetes, extracted from patent WO2009054479A1. | ||||
| GC31698 | PBI-4050 sodium salt (Setogepram (sodium salt)) | 1254472-97-3 | >99.50% | |
Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. | ||||
| GC32481 | Vincamine | 1617-90-9 | >99.50% | |
A plant alkaloid with vasodilator effects | ||||
| GC34464 | AM-4668 | 1011531-27-3 | >99.00% | |
AM-4668 is a GPR40 agonist for type 2 diabetes. | ||||
| GC35313 | AMG 837 calcium hydrate | 1259389-38-2 | >98% | |
AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. | ||||
| GC35314 | AMG 837 sodium salt | 865231-45-4 | >98% | |
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. | ||||
| GC35364 | AP5 | 1623194-37-5 | >98% | |
AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). | ||||
| GC36185 | GPR40 Activator 1 | 1309435-60-6 | >98.50% | |
GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes. | ||||
| GC36507 | LY2922470 | 1423018-12-5 | >99.50% | |
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. | ||||
| GC63010 | HWL-088 | 2378617-96-8 | >98.50% | |
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) . | ||||
