Free Fatty Acid Receptors

Free Fatty Acid (FFA) receptors are a group of Gq/11 protein-coupled receptors currently classified into FFA1, FFA2, FFA3 and FFA4 subtypes. FFA receptors are concentrated in pancreatic islet cells, immune cells and in the brain and are important in immunity and metabolism.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
5789 AM 4668
Potent FFA1 (GPR40) agonist
6082 AMG 837 hemicalcium salt
Potent free fatty acid receptor 1 (FFA1/GPR40) partial agonist
6163 AR 420626
FFA3 agonist
5035 AS 2034178
Selective FFA1 (GPR40) agonist
4642 4-CMTB
FFA2 agonist; also exhibits positive allosteric modulatory activity
4581 Grifolic acid
Selective partial FFA4 (GPR120) agonist
5257 GSK 137647
Potent and selective FFA4 (GPR120) agonist
2649 GW 9508
Potent and selective FFA1 (GPR40) agonist
4615 MEDICA 16
FFA1 (GPR40) agonist; also inhibits ATP citrate lyase
4601 TUG 891
Potent and selective FFA4 (GPR120) agonist
6001 ZQ 16
Selective GPR84 agonist

Antagonists

Cat No Product Name / Activity
5256 AH 7614
Selective FFA4 (GPR120) antagonist
5903 CATPB
FFA2 antagonist/inverse agonist
5357 DC 260126
FFA1 (GPR40) antagonist
5621 GLPG 0974
Potent FFA2 antagonist

Related Targets

    Free Fatty Acid (FFA) receptors are a group of Gq/11 protein-coupled receptors that are currently classified into FFA1, FFA2, FFA3 and FFA4 subtypes. FFA receptors are concentrated in the pancreatic islet cells (particularly FFA1) and in the brain, with lower expression levels found in adipose tissue, peripheral blood mononuclear cells, neutrophils and monocytes.

    FFAs 1, 2 and 3 genes are co-located on chromosome 19 and have closely related sequences, while FFA4 is located on chromosome 10 and has little homology with the other FFAs. FFA1 and FFA4 are activated by long-chain fatty acids (FA), whereas FFA2 and FFA3 are activated by short-chain fatty acids. FFA1 is found principally in pancreatic β cells and is involved in modulation of glucose-stimulated insulin release, while the other FFA receptors are expressed in pancreatic α, β and δ cells. FFA receptors are also expressed in enteroendocrine cells in the gastrointestinal tract where activation by FFA stimulates incretin secretion. FFA2 and FFA4 are additionally expressed in adipose tissue, where they may have a role in obesity, as well as in different immune cells, being involved in regulating inflammatory processes in the gut. FFA3 has a role in modulating inflammatory processes in the airways, and is also expressed in sympathetic ganglia.

    GPR84 is a structurally unrelated G protein-coupled receptor that is putatively activated by medium-chain FA and is found on immune cells, including glial cells, and in adipocytes. Studies suggest a role for GPR84 in inflammatory diseases, such as rheumatoid arthritis and inflammatory bowel disease.

    External sources of pharmacological information for Free Fatty Acid Receptors :

    Literature for Free Fatty Acid Receptors

    GPCR

    GPCR Product Listing

    A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

    • Rhodopsin-like Receptors
    • Secretin-like Receptors
    • Glutamate Receptors
    • Frizzled Receptors
    • GPCR Signaling

    Free Fatty Acid Receptor Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    FFA1 Human FFAR1 NM_005303 O14842
    Mouse Ffar1 NM_194057 Q76JU9
    Rat Ffar1 NM_153304 Q8K3T4
    FFA2 Human FFAR2 NM_005306 O15552
    Mouse Ffar2 NM_146187 Q8VCK6
    Rat Ffar2 NM_001005877 Q76EI6
    FFA3 Human FFAR3 NM_005304 O14843
    Mouse Ffar3 NM_001033316 Q3UFD7
    Rat Ffar3 NM_001108912 XP_006228898
    FFA4 Human FFAR4 NM_181745 Q5NUL3
    Mouse Ffar4 NM_181748 Q7TMA4
    Rat Ffar4 NM_001047088 Q2AC31