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.

Free Fatty Acid Receptor Isoform Specific Products:

Free Fatty Acid Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13967B
    AMG 837 calcium hydrate
    		Agonist 99.00%
    AMG 837 calcium hydrate is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 calcium hydrate stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models. AMG 837 calcium hydrate binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 calcium hydrate can be used in research related to type 2 diabetes and brucellosis.
    AMG 837 calcium hydrate
  • HY-116263
    CATPB
    		99.7%
    CATPB is a potent, selective free fatty acid receptor 2 (FFA2R/GPR43) antagonist.
    CATPB
  • HY-114011
    AMG7703
    		Agonist 99.92%
    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-110390
    GR148672X
    		Inhibitor 99.58%
    GR148672X is an inhibitor of carboxylesterase 1 (CES1) and hepatic microsomal triglyceride hydrolase (TGH). GR148672X blocks the catalytic activity of CES1, impairs the functions of triglyceride and cholesteryl ester lipase, reduces triglyceride mobilization and secretion, and decreases apolipoprotein B-100 secretion in primary rat hepatocytes. Under low-glucose conditions, GR148672X inhibits the survival of colorectal cancer cells by reducing free fatty acid availability, inducing toxic triglyceride accumulation, ROS production, mitochondrial damage, ferroptosis and apoptosis. GR148672X can be used in studies related to colorectal cancer and atherosclerosis.
    GR148672X
  • HY-114610
    13Z,16Z-Docosadienoic acid
    		Agonist 99.00%
    13Z,16Z-Docosadienoic acid is a GPR120 agonist with bactericidal activity. 13Z,16Z-Docosadienoic acid serves as a potential biomarker for canine mammary tumors. 13Z,16Z-Docosadienoic acid is used in the research of bacterial infections, Lyme disease, Graves' disease and mammary tumors.
    13Z,16Z-Docosadienoic acid
  • HY-W009081
    Tricosanoic acid
    		Agonist 99.96%
    Tricosanoic acid is an endogenous agonist of long-chain saturated fatty acids and free fatty acid receptor FFAR1, which can activate hair growth. Tricosanoic acid (C23:0) has the activity of improving cognitive function by regulating neuronal membrane fluidity, inhibiting neuroinflammatory response, participating in myelination and neuronal energy metabolism. Tricosanoic acid expression levels are low in the prefrontal cortex of Alzheimer's disease (AD) models; while better cognitive performance corresponds to higher serum concentration levels. Tricosanoic acid can be used as a biomarker for diseases related to cognitive decline.
    Tricosanoic acid
  • HY-101492
    GPR120 Agonist 3
    		Agonist 99.51%
    GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of 7.62.
    GPR120 Agonist 3
  • HY-147351
    GPR40 agonist 6
    		Agonist 98.81%
    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-19835
    LY2922470
    		Agonist 99.39%
    LY2922470 is a selective and orally active agonist for the G protein-coupled receptor 40 (GPR40). LY2922470 activates GPR40-mediated β-arrestin recruitment with EC50s of 7 nM (human GPR40), 1 nM (mouse GPR40) and 3 nM (rat GPR40). LY2922470 can be used for research 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-147394
    GPR41 agonist-1
    		Agonist 98.04%
    GPR41 agonist-1 (compound 9) is a potent GPR41 agonist. GPR41 agonist-1 can be used for researching insulin-related disorders.
    GPR41 agonist-1
  • HY-15697
    TUG-770
    		Agonist 99.07%
    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-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-103083
    GPR40 agonist 4
    		Agonist 98.05%
    GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
    GPR40 agonist 4
  • HY-123297
    TUG-469
    		Agonist 99.67%
    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-P1123
    MEDICA16
    		Agonist 98.0%
    MEDICA16 is an orally active acetyl-CoA carboxylase and ATP-citrate lyase inhibitor. MEDICA16 limits the acetyl-CoA supply for acetyl-CoA carboxylase, inhibits acetyl-CoA carboxylase activity, exerts citrate-competitive inhibitory effects on ATP-citrate lyase, and reduces hepatic AMPK activity. MEDICA16 can be used in research related to insulin resistance, hyperlipidemia, and obesity.
    MEDICA16
  • HY-Y1624
    1,1'-(Azodicarbonyl)-dipiperidine
    		Agonist ≥98.0%
    1,1'-(Azodicarbonyl)-dipiperidine (ADDP) can be used in the condensation reaction of alcohols with acidic compounds. 1,1'-(Azodicarbonyl)-dipiperidine can also be used in the synthesis of GPR120 agonists with antidiabetic activity, as well as the synthesis of triple agonists for PPARα, PPARγ, and PPARδ. 1,1'-(Azodicarbonyl)-dipiperidine can be used in metabolic disease research.
    1,1'-(Azodicarbonyl)-dipiperidine
  • HY-114060
    CFMB
    		99.95%
    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-119242
    BTI-A-404
    		Inhibitor 99.30%
    BTI-A-404 is a potent, selective and competitive inverse agonist of human GPR43. BTI-A-404 can be used for the research of inflammation, obesity and type 2 diabetes.
    BTI-A-404
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Free Fatty Acid Receptor Isoform Comparison

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