Free Fatty Acid Receptor

Free Fatty Acid Receptor

G protein-coupled receptors (GPCRs) known as free fatty acid receptors (FFARs) are activated by free fatty acids (FFAs). FFAR1/GPR40, FFAR2/GPR43, FFAR3/GPR41, and FFAR4/GPR120 are the four FFARs that have been thoroughly characterized. FFA2 and FFA3 are activated by short chain FFAs, primarily acetate, butyrate, and propionate; FFARs are classified according to the chain length of the FFA ligands that activate each FFAR. FFA1 and GPR120 are activated by medium- or long-chain FFAs, whereas GPR84 is activated by medium-chain FFAs.Each FFAR can therefore function as an FFA sensor with selectivity for a specific FFA carbon chain length derived from food or food-derived metabolites. According to research, FFARs play a variety of physiological roles, including promoting the release of the hormones insulin and incretin, adipocyte differentiation, anti-inflammatory effects, neuronal responses, and taste preferences. It is possible to think of these FFAR physiological functions as regulating immune and energy homeostasis. As a result, therapeutic strategies for the treatment of metabolic disorders like type 2 diabetes and metabolic syndrome have focused on FFARs.

Free Fatty Acid Receptor related products

Structure Cat No. Product Name CAS No. Product Description
V75353 4-CMTB 300851-67-6 4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and positive allosteric modulator (PAM) (pEC50=6.38).
V75354 AMG 837 hemicalcium 1291087-14-3 AMG 837 hemicalcium is a potent, orally bioactive partial agonist of GPR40/FFA1, inhibiting the specific binding of [3H]AMG 837 to the human FFA1 receptor with pIC50 of 8.13.
V2053 AMG-837 calcium hydrate 1259389-38-2 AMG 837 calcium hydrate is a novel, orally bioavailable and potent GPR40 agonist with EC50 of 13 nM and with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
V11531 AR-420626 1798310-55-0 AR-420626 (AR 420626; AR420626) is a novel and potent allosteric agonist of FFA3 (GPR41) receptor (pEC50 value of 5.74) with the potential for the treatment of neurogenic diarrheal disorders by suppressing nAChR-mediated neural pathways.
V75355 BI-2081 1458656-71-7 BI-2081 is a GPR40 (FFAR1) partial agonist (EC50= 4 nM).
V75357 Fasiglifam hemihydrate (TAK-875 hemihydrate) 1374598-80-7 Fasiglifam (TAK-875) hemihydrate is a potent, orally bioactive, selective GPR40 agonist/activator with EC50 of 72 nM.
V3100 GPR120 Agonist 2 1234844-11-1 GPR120 Agonist 2 is a potent and selective agonist of the GPR120 (G-protein coupled receptor) receptor.
V84484 GPR40 agonist 7 1821647-46-4
V28989 GPR40/FFAR1 modulator 1 874755-26-7 GPR40/FFAR1 modulator 1 is an agonist and allosteric modulator of Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
V2812 GSK137647A 349085-82-1 GSK137647A, a diarylsulfonamide analog, is a novel, potent and selective agonists of the free fatty acid receptor 4 (FFA4/GPR120) with pEC50 of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, respectively.
V4937 GW1100 306974-70-9 GW-1100 is a novel, potent and selective GPR40 antagonist with a pIC50 of 6.9. GPR40 has been reported to be activated by long-chain fatty acids, such as docosahexaenoic acid (DHA).
V51355 HWL-088 2378617-96-8 HWL-088 is a port-active fast linker 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM).
V7595 Pinocembrin racemate (DL0108) 68745-38-0 Pinocembrin (DL-0108), the racemate of Pinocembrin, is a potent androgen receptor ligand with the potential for the treatment of acute stroke.
V75356 TP-051 858097-86-6 TP-051 is a potent FFAR1 agonist/activator with a Ki of 16 nM for human FFAR1.
V51362 TUG-499 1206629-08-4 TUG-499 is a cross-coupling related adapter 1 (FFAR1 or GPR40) (free fatty acid receptor) agonist/activator with pEC50 of 7.39.
V3445 TUG-770 1402601-82-4 TUG-770 (TUG770) is a novel, highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40) with EC50 of 6 nM for hFFA1.
V16933 TUG-891 1374516-07-0 TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which displays both potential opportunity and possible challenges to therapeutic agonism.
V5236 Vincamine 1617-90-9 Vincamine is a peripheral vasodilator, that increases blood flow to the brain.
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