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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V114558 | (R)-AM-1638 | 1142222-18-1 | (R)-AM-1638 is the R-isomer of AM-1638. |
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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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V115673 | AS2575959 sodium | 1616871-34-1 | AS2575959 (sodium) is a GPR40 agonist. |
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V115590 | AM-6226 | 1449742-87-3 | AM-6226 is a potent, orally active, full agonist of G protein-coupled receptor 40 (GPR40) with an EC50 of 0.12 μM. |
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V109554 | Tricosanoic acid-d45 | Tricosanoic acid-d45 is a deuterated derivative of tricosanoic acid. | |
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V109530 | Tricosanoic acid-d3 | 2732915-45-4 | Tricosanoic acid-d3 is a deuterated derivative of tricosanoic acid. |
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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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V103985 | FFAR1/FFAR4 agonist-1 | 2839486-16-5 | FFAR1/FFAR4 agonist-1 (Compound 83) is a FFAR1/FFAR4 agonist with EC50 of 1 nM and 4 nM for FFAR1 and FFAR4, respectively. |
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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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