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-162689
    GprA
    		Agonist
    GprA is a new synthetic agonist of G-protein-coupled receptor 120/free fatty acid receptor 4 (GPR120/FFAR4), with an AC50 of 203 nM on human GPR120 full isoform. GprA can be used in the research for NAFLD.
    GprA
  • 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
  • HY-141653
    MK-8666 tromethamine
    		Agonist
    MK-8666 (tromethamine) is a GPR40 agonist. MK-8666 (tromethamine) can be used in the research of type II diabetes.
    MK-8666 tromethamine
  • HY-12413A
    BMS-986118
    		Agonist
    BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC50 of 0.07 µM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models.
    BMS-986118
  • HY-112603A
    AP5 sodium
    		Agonist
    AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research.
    AP5 sodium
  • HY-P1124
    AS2034178 free base
    		Agonist
    AS2034178 free base, a specific and orally active GPR40 agonist, exhibits glucose-dependent insulin secretion enhancement. AS2034178 free base has potential for type 2 diabetes mellitus research.
    AS2034178 free base
  • HY-114060
    CFMB
    CFMB is a full agonist of FFAR2- and FFAR3-specific with EC50 value of 0.8 μM target hFFAR2 and 0.2 μM target rFFAR2.
    CFMB
  • HY-147987
    FFA1 agonist-1
    		Agonist
    FFA1 agonist-1 (Compound 17a) is an orally active fatty acid receptor 1 (FFA1) agonist with an EC50 of 0.75 μM. FFA1 agonist-1 can be used for type 2 diabetes mellitus research.
    FFA1 agonist-1
  • HY-108020
    LY2881835
    		Agonist
    LY2881835 is a potent and selective agonist of G protein-coupled receptor 40 (GPR40). LY2881835 has efficacious and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion. LY2881835 has the potential for the research of type 2 diabetes mellitus. LY2881835 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    LY2881835
  • HY-13971
    GPR40 Activator 1
    		Activator 98.81%
    GPR40 Activator 1 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 Activator 1
  • HY-163530
    GPR41 modulator 1
    		Modulator
    GPR41 modulator 1 (compound 10ak) is a potent GPR41 modulator with an EC50 value of 0.679 µM. GPR41 modulator 1 shows agonistic modulator activity.
    GPR41 modulator 1
  • HY-W010655
    Fasiglifam hemihydrate
    		Activator
    Fasiglifam (TAK-875) hemihydrate is a potent, selective and orally active GPR40 agonist with EC50 of 72 nM. Fasiglifam enhances glucose-dependent insulin secretion and improves hyperglycemia in type 2 diabetic rats. Fasiglifam can induce liver injury.
    Fasiglifam hemihydrate
  • HY-117978
    LY2922083
    		Agonist
    LY2922083 and related compounds LY2881835 and LY2922470 are spiperidine and tetrahydroquinolinic acid derivatives that are potent GPR40 agonists. LY2922083 activates GPR40 in response to elevated blood glucose and has the potential to be a glucose-lowering agent.
    LY2922083
  • HY-N2540R
    (±)-Pinocembrin (Standard)
    (±)-Pinocembrin (Standard) is the analytical standard of (±)-Pinocembrin. This product is intended for research and analytical applications. (±)-Pinocembrin ((±)-5,7-Dihydroxyflavanone) is a GPR120 ligand able to promote wound healing in HaCaT cell line.
    (±)-Pinocembrin (Standard)
  • HY-U00395
    GPR40 Agonist 2
    		Agonist
    GPR40 Agonist 2 is a GPR40 agonist that can be used in the research of diabetes, extracted from patent WO2009054479A1.
    GPR40 Agonist 2
Cat. No. Product Name / Synonyms Application Reactivity