Aleniglipron CAS# 2685823-26-9

Aleniglipron (GSBR-1290) is a potent, orally bioavailable small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonist that activates the Gαs-cAMP signaling pathway with high potency (cAMP EC₅₀ < 0.1 nM) and minimal β-arrestin recruitment, indicating biased agonism. It induced dose-dependent insulin secretion in vitro and improved glucose clearance and insulin release in acute glucose tolerance tests in animals. In rodent and non-human primate models of metabolic disease, oral dosing increased insulin secretion, enhanced glucose control, reduced food intake, and decreased body weight, demonstrating robust metabolic effects consistent with GLP-1R engagement.