2764704-18-7

LSN3318839 is a positive allosteric modulator (PAM) of glucagon-like peptide 1 receptor (GLP-1R).1 It potentiates increases in cAMP accumulation induced by the GLP-1R full agonist GLP-1 (9-36), but not the GLP-1R partial agonist GLP-1 (7-36), in INS-1 832/3 cells. LSN3318839 (1 and 3 µM) increases insulin levels in the presence, but not absence, of GLP-1 (9-36) in INS-1 832/3 cells under high-glucose conditions. It reduces blood glucose levels in glucose-dependent insulinotropic polypeptide receptor (GIPR) knockout mice in an oral glucose tolerance test when administered at a dose of 30 mg/kg and has an additive effect on reducing blood glucose levels in GIPR knockout mice when administered at 10 or 30 mg/kg in combination with the dipeptidyl peptidase 4 (DPP-4) inhibitor sitagliptin.WARNING This product is not for human or veterinary use.

[1] FRANCIS S. WILLARD. Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide-1 Receptor[J]. Journal of Medicinal Chemistry, 2021, 64 6: 3439-3448. DOI: 10.1021/acs.jmedchem.1c00029