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-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-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-135763
    Metabolex-36
    		Agonist
    Metabolex-36 is a FFA4 agonist with a pEC50 value of 5.9 and a pEC50 value of less than 4.0 for FFA1.
    Metabolex-36
  • 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-100881R
    TUG-891 (Standard)
    		Agonist
    TUG-891 (Standard) is the analytical standard of TUG-891. This product is intended for research and analytical applications. TUG-891 is a potent and selective agonist for the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120).
    TUG-891 (Standard)
  • 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-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-W585819
    3-Chloropropane-1,2-diol dipalmitate
    3-Chloropropane-1,2-diol dipalmitate is a free fatty acid consisting mainly of diesters.
    3-Chloropropane-1,2-diol dipalmitate
  • 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-W585819R
    3-Chloropropane-1,2-diol dipalmitate (Standard)
    3-Chloropropane-1,2-diol dipalmitate (Standard) is the analytical standard of 3-Chloropropane-1,2-diol dipalmitate. This product is intended for research and analytical applications. 3-Chloropropane-1,2-diol dipalmitate is a free fatty acid consisting mainly of diesters.
    3-Chloropropane-1,2-diol dipalmitate (Standard)
  • HY-W011303S
    Phytosphingosine-d7
    		Agonist
    Phytosphingosine-d7 (4-Hydroxysphinganine-d7) is deuterium labeled Phytosphingosine. 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-d<sub>7</sub>
  • HY-100775R
    Fezagepras sodium (Standard)
    		Agonist
    Fezagepras (sodium) (Standard) is the analytical standard of Fezagepras (sodium). This product is intended for research and analytical applications. 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 (Standard)
  • 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-100775AR
    Fezagepras (Standard)
    		Agonist
    Fezagepras (Standard) is the analytical standard of Fezagepras. This product is intended for research and analytical applications. 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 (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