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-12940A
    (S)-GLPG0974
    		98.79%
    (S)-GLPG0974 is the isomer of GLPG0974 (HY-12940), and can be used as an experimental control. GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.
    (S)-GLPG0974
  • HY-14363
    TUG-424
    		Agonist ≥98.0%
    TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity. TUG-424 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    TUG-424
  • 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).
    Grifolic acid
  • 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-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-160602
    CPL207280
    		Agonist
    CPL207280 is an orally active GPR40/FFA1 agonist with an antidiabetic effect. CPL207280 can effectively enhance glucose-stimulated insulin secretion and improve glucose tolerance in MIN6 pancreatic β-cells as well as in healthy Wistar Han rats and diabetic rat models. CPL207280 can be used for the research of type 2 diabetes.
    CPL207280
  • 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-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-160628
    GPR120 Agonist 4
    		Agonist
    GPR120 Agonist 4 (example 1) is a GPR120 agonist，with the EC50 values of 1 μM and 0.35 μM for β-arrestin A and Calcium A. GPR120 Agonist 4 can be used for the research of type II diabetes mellitus.
    GPR120 Agonist 4
Cat. No. Product Name / Synonyms Application Reactivity