LSN3318839

LSN3318839 is a positive allosteric modulator (PAM) of glucagon-like peptide 1 receptor (GLP-1R). 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.Formal Name: 2-[1-[(1R)-1-(2,6-dichloro-3-cyclopropylphenyl)ethyl]-1H-imidazo[4,5-c]pyridin-6-yl]-alphaR-methyl-benzeneacetic acid. CAS Number: 2764704-18-7. Molecular Formula: C26H23Cl2N3O2. Formula Weight: 480.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml, DMSO: Sparingly Soluble: 1-10 mg/ml. SMILES: ClC(C(C1CC1)=CC=C2Cl)=C2[C@@H](C)N3C=NC4=CN=C(C=C43)C5=C(C=CC=C5)[C@@H](C)C(O)=O. InChi Code: InChI=1S/C26H23Cl2N3O2/c1-14(26(32)33)17-5-3-4-6-19(17)21-11-23-22(12-29-21)30-13-31(23)15(2)24-20(27)10-9-18(25(24)28)16-7-8-16/h3-6,9-16H,7-8H2,1-2H3,(H,32,33)/t14-,15-/m1/s1. InChi Key: JPJWHCNGSBCZMI-HUUCEWRRSA-N.