TUG-499

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes[1].

Signaling Pathways >> GPCR/G Protein >> GPR40

Research Areas >> Metabolic Disease

pEC50: 7.39 (FFAR1)[1]

TUG-499 (compound 7) demonstrates high chemical stability, no inhibition of selected CYP enzymes or P-glycoprotein, and excellent Caco-2 permeability. TUG-499 has potent activity on recombinant human FFA1 receptors and on the rat insulinoma cell line INS-1E[1].

[1]. Elisabeth Christiansen, et al. Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. J Med Chem. 2011 Oct 13;54(19):6691-703.