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

Free Fatty Acid Receptor

FFAR

Free Fatty Acid Receptor

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-50162
    GPR120 modulator 1
    		Modulator 98.56%
    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.
    GPR120 modulator 1
  • HY-13967
    AMG 837
    		Agonist
    AMG 837 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AMG 837
  • HY-50172
    GPR120 modulator 2
    		Modulator 98.06%
    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.
    GPR120 modulator 2
  • HY-13967A
    AMG 837 sodium salt
    		Agonist
    AMG 837 (sodium salt) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AMG 837 sodium salt
  • 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.
    GPR120 Agonist 1
  • HY-100775A
    Fezagepras
    		Agonist
    Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras decreases renal, liver and pancreatic fibrosis. Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
    Fezagepras
  • HY-111359
    GPR40 agonist 1
    		Agonist
    GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
    GPR40 agonist 1
  • HY-111116
    LY3104607
    		Agonist
    LY3104607 is a potent and selective G protein-coupled receptor 40 (GPR40) agonist. LY3104607 can be used in research of diabetes.
    LY3104607
  • HY-112603
    AP5
    		Agonist
    AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 has the potential for type II diabetes research.
    AP5
  • HY-148247
    BI-2081
    		Agonist
    BI-2081 is a GPR40 (FFAR1) partial agonist (EC50: 4 nM). BI-2081 induces glucose depending insulin secretion and reduces the plasma glucose concentration. BI-2081 can be used in the research of metabolic diseases, in particular diabetes type 2.
    BI-2081
  • HY-129707
    AMG 837 hemicalcium
    		Agonist
    AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.
    AMG 837 hemicalcium
  • HY-16619
    AM-5262
    		Agonist
    AM-5262 is a GPR40 full agonist with an EC50 value of 0.081 μM. AM-5262 can be used for the research of type II diabetes.
    AM-5262
  • HY-148235
    TP-051
    		Agonist
    TP-051 is a potent FFAR1 agonist with an Ki value of 16 nM for human FFAR1. TP-051 can increase insulin secretion in rat insulinoma cells. TP-051 can be used to research type 2 diabetes.
    TP-051
  • HY-114610
    13Z,16Z-Docosadienoic acid
    		Agonist
    13Z,16Z-Docosadienoic acid, a ω-6 polyunsaturated fatty acid, possesses anti-borreliae effect. 13Z,16Z-Docosadienoic acid, as a long-chain fatty acid (LCFA), is a free fatty acid receptor 4 (FFAR4 or GPR120, a LCFA receptor) agonist.
    13Z,16Z-Docosadienoic acid
  • HY-117787
    TUG-905
    		Agonist
    TUG-905 is a potent GPR40 agonist with an pEC50 value of 7.03. TUG-905 increases hypothalamic cell proliferation and survival. TUG-905 reduces body mass and increases the POMC mRNA expression.
    TUG-905
  • HY-119242
    BTI-A-404
    		Inhibitor
    BTI-A-404 is a potent, selective and competitive inverse agonist of human GPR43. BTI-A-404 can be used for the research of inflammation, obesity and type 2 diabetes.
    BTI-A-404
  • HY-121140
    AZ1729
    		Agonist
    AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in Gi-mediated pathways, but not at those transduced by Gq/G11. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2.
    AZ1729
  • 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. GPR40 agonist 5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GPR40 agonist 5
  • HY-162136
    GPR40 agonist 7
    		Agonist
    GPR40 agonist 7 (Compound 1) is an orally active G protein-coupled receptor 40 (GPR40) agonist. GPR40 agonist 7 can significantly increase insulin and GLP-1 secretion, and has a hypoglycemic effect in vivo with an ED50 of 0.58 mg/kg
    GPR40 agonist 7
  • HY-147420
    Xelaglifam
    		Inhibitor
    Xelaglifam is a potent GPR40 agonist. Antihyperglycaemic activity. Xelaglifam is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Xelaglifam
Cat. No. Product Name / Synonyms Application Reactivity