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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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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). |
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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. |
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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. |
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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. |
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V75355 | BI-2081 | 1458656-71-7 | BI-2081 is a GPR40 (FFAR1) partial agonist (EC50= 4 nM). |
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V86602 | CPL207280 | 2361497-72-3 | CPL207280 is an orally active GPR40/FFA1 agonist with anti-diabetic effects. |
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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. |
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V86604 | GPR120 Agonist 4 | 1628641-89-3 | GPR120 Agonist 4 (example 1) is a GPR120 agonist with EC50 values of 1 μM and 0.35 μM for β-arrestin A and Calcium A, respectively. |
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V3100 | GPR120 Agonist 2 | 1234844-11-1 | GPR120 Agonist 2 is a potent and selective agonist of the GPR120 (G-protein coupled receptor) receptor. |
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V84484 | GPR40 agonist 7 | 1821647-46-4 | |
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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). |
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V86603 | GPR41 modulator 1 | GPR41 modulator 1 (compound 10ak) is a potent GPR41 modulator with an EC50 of 0.679 µM. | |
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V86605 | GprA | GprA is a novel synthetic G protein-coupled receptor 120/free fatty acid receptor 4 (GPR120/FFAR4) agonist with an AC50 of 203 nM for the full-length isoform of human GPR120. | |
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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. |
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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). |
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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). |
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V75356 | TP-051 | 858097-86-6 | TP-051 is a potent FFAR1 agonist/activator with a Ki of 16 nM for human FFAR1. |
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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. |
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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. |
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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. |
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