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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)

  • GC10922 structure
    GC10922TUG 424
    CAS: 1082058-99-8
    Purity: >98.00%

    FFA1 (GPR40) agonist

  • GC12401 structure
    GC12401GW9508
    CAS: 885101-89-3
    Purity: >98.00%

    FFA1/GPR40 agonist,potent and selective

  • GC14027 structure
    GC14027GW-1100
    CAS: 306974-70-9
    Purity: >98%

    A selective GPR40 antagonist

  • GC16054 structure
    GC16054TUG-770
    CAS: 1402601-82-4
    Purity: >99.50%

    An agonist of FFA1/GPR40

  • GC16555 structure
    GC16555TAK-875
    CAS: 1000413-72-8
    Purity: >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 structure
    GC18125DC260126
    CAS: 346692-04-4
    Purity: >98.00%

    free fatty acid receptor 1 (FFAR1/GPR40) antagonist

  • GC19030 structure
    GC19030AMG 837
    CAS: 865231-46-5
    Purity: >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 structure
    GC31389GPR40 Activator 2
    CAS: 1312787-30-6
    Purity: >99.50%

    GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.

  • GC31410 structure
    GC31410FAA1 agonist-1
    CAS: 2102196-57-4
    Purity: >98.50%

    FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.

  • GC31607 structure
    GC31607AM-1638
    CAS: 1142214-62-7
    Purity: >99.50%

    AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.

  • GC31634 structure
    GC31634GPR40 Agonist 2
    CAS: 1147729-48-3
    Purity: >98%

    GPR40 Agonist 2 is a GPR40 agonist that can be used in the research of diabetes, extracted from patent WO2009054479A1.

  • GC31698 structure
    GC31698PBI-4050 sodium salt (Setogepram (sodium salt))
    CAS: 1254472-97-3
    Purity: >99.50%

    Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84.

  • GC32481 structure
    GC32481Vincamine
    CAS: 1617-90-9
    Purity: >99.50%

    A plant alkaloid with vasodilator effects

  • GC34464 structure
    GC34464AM-4668
    CAS: 1011531-27-3
    Purity: >99.00%

    AM-4668 is a GPR40 agonist for type 2 diabetes.

  • GC35313 structure
    GC35313AMG 837 calcium hydrate
    CAS: 1259389-38-2
    Purity: >98%

    AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1.

  • GC35314 structure
    GC35314AMG 837 sodium salt
    CAS: 865231-45-4
    Purity: >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 structure
    GC35364AP5
    CAS: 1623194-37-5
    Purity: >98%

    AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM).

  • GC36185 structure
    GC36185GPR40 Activator 1
    CAS: 1309435-60-6
    Purity: >98.50%

    GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.

  • GC36507 structure
    GC36507LY2922470
    CAS: 1423018-12-5
    Purity: >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 structure
    GC63010HWL-088
    CAS: 2378617-96-8
    Purity: >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) .