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-19835
    LY2922470
    		Agonist 99.11%
    LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM).
    LY2922470
  • HY-19995
    GSK137647A
    		Agonist 99.81%
    GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response.
    GSK137647A
  • HY-116263
    CATPB
    		≥99.0%
    CATPB is a potent, selective free fatty acid receptor 2 (FFA2R/GPR43) antagonist.
    CATPB
  • HY-132265
    SCO-267
    		Agonist 99.31%
    SCO-267 is an allosteric GPR40 full agonist. SCO-267 can be used for the research of chronic diseases including diabetes.
    SCO-267
  • HY-101492
    GPR120 Agonist 3
    		Agonist 99.20%
    GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of ?7.62.
    GPR120 Agonist 3
  • HY-15697
    TUG-770
    		Agonist 99.35%
    TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research. TUG-770 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-770
  • HY-P1123
    MEDICA16
    		Agonist ≥98.0%
    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.
    MEDICA16
  • HY-103083
    GPR40 agonist 4
    		Agonist 98.38%
    GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
    GPR40 agonist 4
  • HY-111763
    GPR40/FFAR1 modulator 1
    		Agonist 99.11%
    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
    GPR40/FFAR1 modulator 1
  • HY-130120
    HWL-088
    		Agonist 98.61%
    HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.
    HWL-088
  • HY-100775A
    Fezagepras
    		Agonist 99.38%
    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-123297
    TUG-469
    		Agonist 99.90%
    TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes.
    TUG-469
  • HY-147351
    GPR40 agonist 6
    		Agonist 99.64%
    GPR40 agonist 6 (Compound 7a) is a potent and selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist with an EC50 of 0.058 μM.
    GPR40 agonist 6
  • HY-136896
    FFA3 agonist 1
    		Agonist
    FFA3 agonist 1 is an agonist of free fatty acid receptor 3 (FFA3). FFA3 agonist 1 regulates the health effect of intestinal microbiota by activating FFA3.
    FFA3 agonist 1
  • HY-148418
    TUG-499
    		Agonist 99.78%
    TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes. TUG-499 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-499
  • 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-114610
    13Z,16Z-Docosadienoic acid
    		Agonist 99.00%
    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-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
Cat. No. Product Name / Synonyms Application Reactivity