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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. 产品名称 Information
  2. GC63010 HWL-088 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。
  3. GC36507 LY2922470

    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。

  4. GC36185 GPR40 Activator 1 GPR40 Activator 1是GPR40活化剂,可作用于2型糖尿病。
  5. GC35364 AP5 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。
  6. GC35314 AMG 837 sodium salt An FFAR1 (GPR40) partial
  7. GC35313 AMG 837 calcium hydrate An FFAR1 (GPR40) partial
  8. GC34464 AM-4668

    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。

  9. GC32481 Vincamine

    长春胺

    A plant alkaloid with vasodilator effects
  10. GC31698 PBI-4050 sodium salt (Setogepram (sodium salt))

    Setogepram sodium; PBI-4050 sodium

    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。
  11. GC31634 GPR40 Agonist 2 GPR40Agonist2是GPR40激动剂,可用于糖尿病的研究。
  12. GC31607 AM-1638 AM-1638是有效,有口服活性的GPR40/FFA1激动剂,EC50值为0.16μM。
  13. GC31410 FAA1 agonist-1 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。
  14. GC31389 GPR40 Activator 2 GPR40Activator2是一出自专利的GPR40激动剂,WO2012147516A1,WO2012046869A1和WO2011078371A1。
  15. GC19030 AMG 837

    (BETAS)-BETA-1-丙炔-1-基-4-[[4'-(三氟甲基)[1,1'-联苯]-3-基]甲氧基]苯丙酸

    An FFAR1 (GPR40) partial
  16. GC18125 DC260126 An FFAR1 (GPR40) antagonist
  17. GC10922 TUG 424 A selective FFAR1 (GPR40) agonist
  18. GC16555 TAK-875

    TAK 875;TAK875

    A selective FFAR1 (GPR40) agonist
  19. GC12401 GW9508 An agonist of GPR40
  20. GC16054 TUG-770

    TUG770;TUG 770

    An agonist of FFA1/GPR40
  21. GC14027 GW-1100

    GW1100;GW1100

    A selective GPR40 antagonist

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