1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR40

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.

GPR40 相关产品 (17):

Cat. No. Product Name Effect Purity
  • HY-10480
    Fasiglifam Activator 98.94%
    Fasiglifam (TAK-875) 是一种有效的,可口服的,具有选择性的 GPR40 激动剂,EC50 值为 72 nM。
  • HY-50691
    GW-1100 Antagonist
    GW-1100是选择性的 GPR40 拮抗剂,pIC50为6.9。
  • HY-15589
    GW9508 Agonist 99.19%
    GW9508是FFA1(GPR40)激动剂,pEC50为7.32,比对GPR120的抑制性高100倍,可通过葡萄糖敏感的方式刺激胰岛素分泌。
  • HY-100775
    PBI-4050 sodium salt Agonist 99.39%
    PBI-4050 用作 GPR40 激动剂和 GPR84 拮抗剂或反向激动剂。
  • HY-101906
    DC260126 Antagonist 99.70%
    DC260126 是一种 GPR40 拮抗剂。
  • HY-112603
    AP5 Agonist
    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。
  • HY-111359
    GPR40 agonist 1 Agonist
    GPR40 agonist 1是有效,新颖的 GPR40 激动剂,对hGPR40 和 rGPR40的EC50 分别为 2 nM 和 17 nM。
  • HY-111763
    GPR40/FFAR1 modulator 1 Agonist
    GPR40/FFAR1 modulator 1 是一种 Gq 偶联游离脂肪酸受体 1 GPR40/FFAR1 的激动剂,也是其别构调节剂。
  • HY-12647
    GPR40 Activator 2 Activator 99.63%
    GPR40 Activator 2是一出自专利的GPR40激动剂,WO 2012147516 A1,WO 2012046869A1和WO 2011078371 A1。
  • HY-103083
    FAA1 agonist-1 Agonist 98.97%
    FAA1 agonist-1 是一个强效的游离脂肪酸受体 1 (FFA1/GPR40) 激动剂,其 pEC50 值为 7.54。
  • HY-13967
    AMG 837 Agonist
    AMG 837钠盐是GPR40激动剂,EC50为13 nM,具有较好的药代动力学表现。
  • HY-13967B
    AMG 837 calcium hydrate Agonist 98.01%
    AMG 837氢氧化钙是GPR40激动剂,EC50为13 nM,具有较好的药代动力学表现。
  • HY-13967A
    AMG 837 sodium salt Agonist
    AMG 837钠盐是GPR40激动剂,EC50为13 nM,具有较好的药代动力学表现。
  • HY-15697
    TUG-770 Agonist 98.52%
    TUG-770是游离脂肪酸受体1(FFA1/GPR40)激动剂,对hFFA1的EC50为6 nM。
  • HY-13971
    GPR40 Activator 1 Activator
    GPR40 Activator 1是GPR40活化剂,可作用于2型糖尿病。
  • HY-13467
    AM-1638 Agonist
    AM-1638是有效,有口服活性的 GPR40/FFA1 激动剂,EC50 值为0.16 μM。
  • HY-U00395
    GPR40 Agonist 2 Agonist
    GPR40 Agonist 2 是 GPR40 激动剂,可用于糖尿病的研究。
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