AR231453

Synthetic agonist of the orphan GPR119. Although endogenous lipid amides such as oleoyl ethanolamide have been reported to be agonists at GPR119, AR231453 is the first reported high potency agonist (EC₅₀=0.68nM). The compound displayed in vivo activity in rodents and was active in an oral glucose tolerance test in mice following oral administration. AR231453 stimulated the release of GLP-1 via GPR119 receptors in mouse models. It was shown to be a highly selective ligand with no off-target activity across a 76 receptor and enzyme profiling panel (CEREP) and no activity against 140 known and orphan GPCRs in melanophore dispersion assays.