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.

FFAR1 (GPR40) 相关产品(20)

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

    A selective FFAR1 (GPR40) agonist

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

    An agonist of GPR40

  • GC14027 structure
    GC14027GW-1100
    CAS: 306974-70-9

    A selective GPR40 antagonist

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

    An agonist of FFA1/GPR40

  • GC16555 structure
    GC16555TAK-875
    CAS: 1000413-72-8
    纯度: >98.50%

    TAK-875是一种有效的,高选择性的口服生物利用的GPR40(G蛋白偶联受体40)激动剂,对人GPR40的EC 50 值为0.014μM。

  • GC18125 structure
    GC18125DC260126
    CAS: 346692-04-4
    纯度: >98.00%

    An FFAR1 (GPR40) antagonist

  • GC19030 structure
    GC19030AMG 837
    CAS: 865231-46-5

    An FFAR1 (GPR40) partial

  • GC31389 structure
    GC31389GPR40 Activator 2
    CAS: 1312787-30-6
    纯度: >99.50%

    GPR40Activator2是一出自专利的GPR40激动剂,WO2012147516A1,WO2012046869A1和WO2011078371A1。

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

    FAA1 agonist-1 是一种有效的游离脂肪酸受体 1 (FFA1/ GPR40) 激动剂,pEC50 为 7.54。

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

    AM-1638是有效,有口服活性的GPR40/FFA1激动剂,EC50值为0.16μM。

  • GC31634 structure
    GC31634GPR40 Agonist 2
    CAS: 1147729-48-3

    GPR40Agonist2是GPR40激动剂,可用于糖尿病的研究。

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

    Fezagepras (Setogepram) sodium 作为 GPR40 的口服活性激动剂和 GPR84 的拮抗剂或反向激动剂。

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

    A plant alkaloid with vasodilator effects

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

    AM-4668是一种GPR40激动剂,用于2型糖尿病研究。在A9细胞中和CHO细胞,激活GPR40的EC50分别为3.6nM和36nM。

  • GC35313 structure
    GC35313AMG 837 calcium hydrate
    CAS: 1259389-38-2

    An FFAR1 (GPR40) partial

  • GC35314 structure
    GC35314AMG 837 sodium salt
    CAS: 865231-45-4

    An FFAR1 (GPR40) partial

  • GC35364 structure
    GC35364AP5
    CAS: 1623194-37-5

    AP5 是一种有效的选择性 GPR40 受体激动剂,在大鼠 hIP1 实验中,AP5 作用于 GPR40 受体,EC50 为 0.49±0.28 nM。

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

    GPR40 Activator 1是GPR40活化剂,可作用于2型糖尿病。

  • GC36507 structure
    GC36507LY2922470
    CAS: 1423018-12-5
    纯度: >99.50%

    LY2922470 是一种有效、选择性的,口服有效的 GPR40 激动剂,作用于 人 GPR40、小鼠 GPR40、大鼠 GPR40 的 EC50 值分别为 7 nM、1 nM、3 nM。LY2922470 可降低血糖水平,同时显著增加胰岛素和 GLP-1,具有治疗 2 型糖尿病 (T2DM) 的潜力。

  • GC63010 structure
    GC63010HWL-088
    CAS: 2378617-96-8
    纯度: >98.50%

    HWL-088 是一种高效的,具有口服活性的游离脂肪酸受体 1 (FFA1/GPR40) 激动剂 (EC50 为 18.9 nM),并具有中等 PPARδ 活性 (EC50 为 570.9 nM)。HWL-088 改善葡萄糖和脂质代谢,并具有抗糖尿病作用。