1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR120

GPR120

GPR120 (Free fatty acid receptor 4, FFA4) is a G protein-coupled receptor that acts as a sensor of long-chain fatty acids, modulates metabolism, and whose dysfunction participates in endocrine disturbances. In humans, two isoforms, long and short, of GPR120 receptors have been reported. Human GPR120 receptors couples with Gαq/11 and activates phospholipase C, leading to the hydrolysis of phosphatidylinositol 4, 5-bisphosphate, generating inositol trisphosphate and diacylglycerol. Inositol trisphosphate triggers calcium release from intracellular stores, whereas diacylglycerol, together with calcium, activates protein kinase C.

GPR120 has been shown to be densely expressed in human lungs and colon, as well as in adipocytes and macrophages, where it recognizes long-chained FFAs including palmitic acid, oleic acid, myristic acid, and importantly, the family of polyunsaturated omega-3 fatty acids, including α-linolenic acid (ALA), eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA). Agonism of GPR120 has been shown to mediate endocrine processes including secretion of glucagon-like peptide-1 (GLP-1) and cholecystokinin from intestinal enteroendocrine cells, inhibition of ghrelin secretion from gastric ghrelin cells, and regulation of adipocyte differentiation. GPR120 agonism has been shown to modulate numerous anti-inflammatory and insulin-sensitizing effects including suppression of TNF-α and IL-6 secretion from macrophages and enhancement of GLUT4 translocation and glucose uptake in adipocytes. GPR120 is a potential novel therapeutic target for the treatment of type 2 diabetes mellitus (T2DM).

GPR120 Related Products (11):

Cat. No. Product Name Effect Purity
  • HY-100881
    TUG-891
    Agonist 99.20%
    TUG-891 is a potent and selective agonist for the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120).
  • HY-19995
    GSK137647A
    Agonist 99.51%
    GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.
  • HY-19996
    AH-7614
    Antagonist ≥99.0%
    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-101492
    GPR120 Agonist 3
    Agonist 99.08%
    GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of −7.62.
  • HY-N0040
    Ginsenoside Rb2
    Activator ≥98.0%
    Ginsenoside Rb2 is one of the main bioactive components of ginseng extracts. Rb2 can upregulate GPR120 gene expression. Ginsenoside Rb2 has antiviral effects.
  • HY-111353
    GPR120 Agonist 2
    Agonist 99.07%
    GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
  • HY-N3977
    Grifolic acid
    Agonist ≥98.0%
    Grifolic acid is a phenolic compound that is first extracted from the mushroom Albatrellus confluens. Grifolic acid acts as an agonist of the free fatty acid receptor (FFAR4/GPR120).
  • HY-50162
    GPR120 modulator 1
    Modulator 98.62%
    GPR120 modulator 1 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F1. GPR120 modulator 1 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes.
  • HY-50172
    GPR120 modulator 2
    Modulator
    GPR120 modulator 2 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F13. GPR120 modulator 2 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes.
  • HY-108711
    GPR120 Agonist 1
    Agonist
    GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate.
  • HY-P1123
    MEDICA16
    Agonist
    MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120.
Isoform Specific Products

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