1. Signaling Pathways
  2. GPCR/G Protein
  3. Free Fatty Acid Receptor

Free Fatty Acid Receptor

Free fatty acid receptors (FFARs) are G protein-coupled receptors (GPCRs) activated by free fatty acids (FFAs). The four well-characterized FFARs are FFAR1/GPR40, FFAR2/GPR43, FFAR3/GPR41, and FFAR4/GPR120. FFARs are categorized according to the chain length of FFA ligands that activate each FFAR; FFA2 and FFA3 are activated by short chain FFAs, mainly acetate, butyrate, and propionate. GPR84 is activated by medium-chain FFAs, whereas FFA1 and GPR120 are activated by medium- or long-chain FFAs. Thus, each FFAR can act as an FFA sensor with selectivity for a particular FFA carbon chain length derived from food or food derived metabolites. FFARs have been reported to have physiological functions such as facilitation of insulin and incretin hormone secretion, adipocyte differentiation, anti-inflammatory effects, neuronal responses, and taste preferences. These physiological functions of FFARs could be considered to regulate energy and immune homeostasis. Therefore, FFARs have been targeted in therapeutic strategies for the treatment of metabolic disorders including type 2 diabetes and metabolic syndrome.

Free Fatty Acid Receptor Related Products (46):

Cat. No. Product Name Effect Purity
  • HY-10480
    Fasiglifam
    Activator 98.94%
    Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.
  • HY-100881
    TUG-891
    Agonist 99.36%
    TUG-891 is a potent and selective agonist for the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120).
  • HY-50691
    GW-1100
    Antagonist
    GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.
  • HY-15589
    GW9508
    Agonist 99.64%
    GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
  • HY-19996
    AH-7614
    Antagonist 99.64%
    AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist.
  • HY-N2540
    (±)-Pinocembrin
    (±)-Pinocembrin ((±)-5,7-Dihydroxyflavanone) is a GPR120 ligand able to promote wound healing in HaCaT cell line.
  • HY-147678
    GPR40 agonist 5
    Agonist
    GPR40 agonist 5 (compound I-14) is an orally active and potent GPR40 (G protein coupled receptor 40) agonist, with an EC50 of 47 nM. GPR40 agonist 5 decreases the levels of blood glucose and improves the glucose tolerance. GPR40 agonist 5 has sufficient effectiveness for the control of hyperglycemia state in type 2 diabetic mice.
  • HY-147420
    Xelaglifam
    Inhibitor
    Xelaglifam is a potent GPR40 agonist. Antihyperglycaemic activity.
  • HY-101906
    DC260126
    Antagonist 99.74%
    DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively). DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis.
  • HY-P1125
    4-CMTB
    99.35%
    4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38).
  • HY-100775
    Fezagepras sodium
    Agonist 99.65%
    Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras sodium decreases renal, liver and pancreatic fibrosis. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
  • HY-13467
    AM-1638
    Agonist 99.67%
    AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
  • HY-101492
    GPR120 Agonist 3
    Agonist 99.42%
    GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of −7.62.
  • HY-N0040
    Ginsenoside Rb2
    98.26%
    Ginsenoside Rb2 is one of the main bioactive components of ginseng extracts. Rb2 can upregulate GPR120 gene expression. Ginsenoside Rb2 has antiviral effects.
  • HY-19995
    GSK137647A
    Agonist 99.88%
    GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response.
  • HY-19835
    LY2922470
    Agonist 99.87%
    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. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM).
  • HY-112813
    TUG-1375
    99.60%
    TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
  • HY-15697
    TUG-770
    Agonist 99.59%
    TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research.
  • HY-B1021
    Vincamine
    Agonist 99.76%
    Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation. Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research.
  • HY-103083
    GPR40 agonist 4
    Agonist 98.69%
    GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
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