ffa2

FFA2 agonist-1 (Compound 4) is an agonist of the free fatty acid receptor 2 (FFA2 GPR43) with an EC50 of 81 nM. It demonstrates activity in β-arrestin-2 recruitment and cAMP inhibition assays, with EC50 values of 1.2 μM and 0.53 μM, respectively. FFA2 agonist-1 can induce the mucosal response of appetite-regulating peptide YY (PYY), inhibit fat accumulation, and affect intestinal function and food intake, making it useful for obesity research.

GLPG0974 is an antagonist of FFA2 GPR43 with IC50 of 9 nM.

GSK137647A (GSK 137647) is a selective agonist of FFA4.

TUG-1375 is an Agonist of Thiazolidine Free Fatty Acid Receptor 2

4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist (EC50: 7.39). It shows higher affinity for FFAR1 or GPR40 relative to related receptors FFA2, FFA3, and the nuclear receptor PPARγ, as well as various other receptors, ion channels, and transporter proteins. TUG-499 is useful for studying Type 2 diabetes.

CFMB is the FFA2 receptor agonist.

TUG-1609 is a fluorescent tracer of FFA2 with good spectral properties and high affinity.

FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. J.Biol.Chem. 291 18915 PMID:27385588 |Sergeev et al (2017) A single extracellular amino acid in free fatty acid receptor 2 defines antagonist species selectivity and G protein selection bias. Sci.Rep. 7 13741 PMID:29061999

LCRF-0004 is a potent and selective RON receptor tyrosine kinase inhibitor. The RON receptor tyrosine kinase has been identified as an important mediator of KRAS oncogene addiction and is overexpressed in the majority of pancreatic cancers. Preclinical studies show that inhibition of RON function decreases pancreatic cancer cell migration, invasion, and survival and can sensitize pancreatic cancer cells to chemotherapy. RON receptor tyrosine kinase is a potential as a therapeutic target.

LON63114, also known as FFA2-Agonist-1 is a selective orthosteric agonist of human FFA2. FFA2-Agonist-1 is potentially useful in the treatment of gastrointestinal disorders and inflammatory bowel diseases. LON63114 was reported in WO2011076732. This product has no formal name at the moment. For the convenience of communication, a temporal code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https: www.medkoo.com page naming).

MOMBA is a selective orthosteric agonist specifically targeting engineered human free fatty acid 2 (hFFA2) receptors, particularly those modified as designer receptors activated by designer drugs (DREADD). It demonstrates selective inactivity towards wild-type hFFA2, hFFA3, and mouse FFA2 receptors. It efficiently inhibits forskolin-induced cAMP levels in cells equipped with the hFFA2-DREADD receptor, exhibiting enhanced potency and comparable efficacy to Sorbic acid. In transgenic mice containing the hFFA2-DREADD gene, MOMBA administration notably slows gut transit and facilitates a concentration-dependent enhancement of GLP-1 secretion from colonic crypts, all while being orally bioavailable.