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-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-P1123R
    MEDICA16 (Standard)
    		Agonist
    Tacrine (hydrochloride) (Standard) is the analytical standard of Tacrine (hydrochloride). This product is intended for research and analytical applications. Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease.
    MEDICA16 (Standard)
  • HY-N0040R
    Ginsenoside Rb2 (Standard)
    Ginsenoside Rb2 (Standard) is the analytical standard of Ginsenoside Rb2. This product is intended for research and analytical applications. Ginsenoside Rb2 is one of the main bioactive components of ginseng extracts. Rb2 can upregulate GPR120 gene expression. Ginsenoside Rb2 has antiviral effects.
    Ginsenoside Rb2 (Standard)
  • 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-109692
    GPR120 Agonist 5
    		Agonist
    GPR120 Agonist 5 (compound 12) is an agonist targeting GPR120 (EC50=1.2 μM). GPR120 Agonist 5 promotes the release of glucagon-like 1 (GLP-1) by binding to the GPR120 receptor, which in turn binds to its receptors on pancreatic beta cells, increasing insulin secretion and thereby lowering blood sugar levels. GPR120 Agonist 5 also helps reduce chronic low-grade inflammation, which plays an important role in the pathogenesis of obesity, insulin resistance, and type 2 diabetes. GPR120 Agonist 5 can be used to investigate the mechanism of action of GPR120 in metabolic and inflammatory diseases.
    GPR120 Agonist 5
  • HY-171069
    FFA2 agonist-1
    		Agonist
    FFA2 agonist-1 (Compound 4) is the agonist for Free fatty acid receptor 2 (FFA2/GPR43) with an EC50 of 81 nM. FFA2 agonist-1 exhibits activity in β-arrestin-2 recruitment assay and cAMP inhibition assay with EC50 of 1.2 μM and 0.53 μM. FFA2 agonist-1 leads to appetite regulating peptide YY (PYY) mucosal responses, inhibits the fat accumulation, intestinal functions and food intake, and can be used for obesity research.
    FFA2 agonist-1
  • HY-B1021R
    Vincamine (Standard)
    		Agonist
    Vincamine (Standard) is the analytical standard of Vincamine. This product is intended for research and analytical applications. Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation. Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research.
    Vincamine (Standard)
  • HY-129136
    TUG-1387
    		Control 98.67%
    TUG-1387 is a control compound for the FFA4 antagonists AH-7614 (HY-19996) and TUG-1506 without inhibitroy activity against FFA4. TUG-1387 can be used as a negative control for FFA4 functional assessments.
    TUG-1387
  • 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
  • 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-164870
    FFAR1/FFAR4 agonist-1
    		Agonist
    FFAR1/FFAR4 agonist-1 (compound 83) is a FFAR1/FFAR4 agonist with the EC50 of 1 nM A and 4nM for FFAR1 and FFAR4, respectively. FFAR1/FFAR4 agonist-1 can be used for study of glycemic control.
    FFAR1/FFAR4 agonist-1
  • HY-125603
    Termitomycamide B
    Termitomycamide B (compound 2) is a neuroprotective agent that can be obtained from Termitomyces titanicus. Termitomycamide B effectively inhibits endoplasmic reticulum stress-dependent cell death. Termitomycamide B can be used in the study of neurodegenerative diseases.
    Termitomycamide B
  • 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
Cat. No. Product Name / Synonyms Application Reactivity