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-12940
    GLPG0974
    		98.56%
    GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.
    GLPG0974
  • HY-10480
    Fasiglifam
    		Activator 98.94%
    Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.
    Fasiglifam
  • HY-50691
    GW-1100
    		Antagonist
    GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.
    GW-1100
  • HY-100881
    TUG-891
    		Agonist 99.47%
    TUG-891 is a potent and selective agonist for the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120).
    TUG-891
  • HY-19996
    AH-7614
    		Antagonist 99.73%
    AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist.
    AH-7614
  • 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-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-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-15589
    GW9508
    		Agonist 99.33%
    GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
    GW9508
  • HY-116522
    AR420626
    		Agonist 98.29%
    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC50=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca2+ signal-mediated glucose uptake and improve diabetes.
    AR420626
  • HY-W011303
    Phytosphingosine
    		Agonist ≥98.0%
    Phytosphingosine is a phospholipid with anti-inflammatory, antibacterial, and anti-cancer activities, which can induce apoptosis. Phytosphingosine is an immune regulator and can be used in the study of inflammatory skin diseases. Phytosphingosine is also an activator of GPR120 with an IC50 value of 33.4 μM and can be used in the study of type II diabetes.
    Phytosphingosine
  • HY-P1125
    4-CMTB
    		99.64%
    4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38).
    4-CMTB
  • HY-101906
    DC260126
    		Antagonist 99.74%
    DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively). DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis.
    DC260126
  • HY-112813
    TUG-1375
    		99.42%
    TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
    TUG-1375
  • HY-N0040
    Ginsenoside Rb2
    		98.26%
    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
  • HY-13467
    AM-1638
    		Agonist 99.65%
    AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
    AM-1638
  • HY-100775
    Fezagepras sodium
    		Agonist 99.65%
    Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras sodium decreases renal, liver and pancreatic fibrosis. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
    Fezagepras sodium
  • HY-114011
    AMG7703
    		Agonist 99.24%
    AMG7703 is a selective and allosteric agonists of FFA2 (GPR43), the receptor for short-chain fatty acids (SCFAs), acetate, and propionate. AMG7703 can be used to research for in inflammatory and metabolic.
    AMG7703
  • HY-13967B
    AMG 837 calcium hydrate
    		Agonist 98.45%
    AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents. AMG 837 (calcium hydrate) 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 calcium hydrate
  • HY-B1021
    Vincamine
    		Agonist 99.65%
    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
Cat. No. Product Name / Synonyms Application Reactivity