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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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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V136869 | GPR40 Activator 3 | 2980-31-6 | GPR40 Activator 3 is a powerful GPR40 activator. |
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V84484 | GPR40 agonist 7 | 1821647-46-4 | |
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V136871 | GPR40 agonist 9 | 1877252-91-9 | GPR40 agonist 9 is a G protein-coupled receptor 40 (GPR40) agonist with an EC50 of 0.21 nM. |
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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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V136872 | GPR41 modulator 2 | 3050769-11-1 | GPR41 modulator 2 (compound 10bx) has agonistic activity against the G protein-coupled receptor (GPR41). |
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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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V119052 | LXT34 | 1609286-95-4 | LXT34 (Example 2) is a GPR120 agonist. |
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V114976 | MK-8666 | 1544739-75-4 | MK-8666 is a potent and selective partial GPR40 agonist (EC50 for human GPR40 is 0.54 nM). |
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V105572 | MOMBA | 6880-04-2 | MOMBA is a selective orthosteric agonist of FFA2 (free fatty acid receptor 2) that activates the receptor signaling pathway by binding to the orthosteric site of FFA2 with high specificity. |
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V141044 | NBSI | 2174014-78-7 | |
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V142902 | PODi-1 | 169454-15-3 | |
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V144215 | RL450 | ||
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V144216 | RL480 | ||
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V144217 | RL560 | ||
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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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