FFA
Free fatty acids (FFAs) are essential nutrients. An ever-increasing number of studies have demonstrated that FFAs are important signaling molecules as well, contributing to many cellular functions. FFAs have been found to activate several G protein–coupled receptors (GPCRs), which are named free fatty acid receptors (FFARs), including G protein–coupled receptor 40 (GPR40 aka FFAR1), GPR41 (FFAR3), GPR43 (FFAR2), GPR84, GPR119, and GPR120 (FFAR4)[1]. The FFAR’s are a critical component of the body’s nutrient sensing apparatus, and small molecule agonists and antagonists of these receptors show considerable promise in the management of obesity, dyslipidemia, and diabetes. Unlike the classic ‘lock and key’ relationship between receptors and their ligands, nutrient receptors are considered to be promiscuous in that they can be activated by a range of ligands[2].
[1] Q Zhang et al. Discovery and Characterization of a Novel Small-Molecule Agonist for Medium-Chain Free Fatty Acid Receptor G Protein-Coupled Receptor 84. J Pharmacol Exp Ther. 2016 May;357(2):337-44.
[2] Free fatty acid receptors: emerging targets for treatment of diabetes and its complications V. Vangaveti, V. Shashidhar, G. Jarrod, B.T. Baune, R.L. Kennedy. Ther. Adv. Endocrinol. Metab. 2010, 1, 165-175.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2405 | AMG 837 calcium | Orally bioavailable partial agonist of GPR40 (FFA1) | €90.00 | |
| 2794 | AR 420626 | GPR41 receptor agonist (FFA3) | €95.00 | |
| 3057 | DC260126 | GPR40 receptor antagonist (FFA1) | €65.00 | |
| 2582 | GSK 137647A | Potent and selective FFA4/GPR120 agonist | €70.00 | |
| 2013 | GW 9508 | GPR40 receptor agonist (FFA1) | €85.00 | |
| 2075 | TUG 891 | Potent and selective GPR120 (FFA4) agonist | €110.00 | |
| 3078 | TUG-1375 | Potent GPR43 receptor agonist (FFA2) | €180.00 | |
| 2616 | ZQ-16 | Potent and selective GPR84 agonist that induces phosphorylation of ERK1/2 | €95.00 | |