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

Free Fatty Acid Receptor

FFAR

Free Fatty Acid Receptor

Related Products

PDF 0.36 MB

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 98.06%
    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-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.
    GPR120 modulator 2
  • HY-12585
    AM-4668
    		Agonist ≥99.0%
    AM-4668 is a GPR40 agonist for type 2 diabetes. EC50s of 3.6 nM and 36 nM for GPR40 in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), respectively.
    AM-4668
  • HY-N2540
    (±)-Pinocembrin
    		99.60%
    (±)-Pinocembrin ((±)-5,7-Dihydroxyflavanone) is a GPR120 ligand able to promote wound healing in HaCaT cell line.
    (±)-Pinocembrin
  • HY-12647
    GPR40 Activator 2
    		Activator 99.63%
    GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
    GPR40 Activator 2
  • HY-111353
    GPR120 Agonist 2
    		Agonist 99.07%
    GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
    GPR120 Agonist 2
  • HY-121140
    AZ1729
    		Agonist 99.8%
    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-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-10480A
    (R)-Fasiglifam
    		Control 98.95%
    (R)-Fasiglifam is the isomer of Fasiglifam (HY-10480), and can be used as an experimental control. Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.
    (R)-Fasiglifam
  • 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-119546
    Pinolenic acid
    		Agonist ≥98.0%
    Pinolenic acid (PNLA) is a polyunsaturated fatty acid that can be isolated from Pinus orientalis and Pinus pinaster seed oil. Pinolenic acid has anti-inflammatory and lipid-lowering activities.
    Pinolenic acid
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity