Formulation: A solid
Formal Name: 3-[(1S,2S)-1-[2-[[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2,3-dihydro-2-oxo-1H-imidazol-1-yl]-2,4,6,7-tetrahydro-4-methyl-5H-pyrazolo[4,3-c]pyridin-5-yl]carbonyl]-5-[(4S)-tetrahydro-2,2-dimethyl-2H-pyran-4-yl]-1H-indol-1-yl]-2-methylcyclopropyl]-1,2,4-oxadiazol-5(2H)-one
Purity: ≥95%
Formula Markup: C48H48F2N10O5
Formula Weight: 883
Shelf life (days): 1460
CAS Number: 2212020-52-3
Notes: Orforglipron is a nonpeptide agonist of the glucagon-like peptide 1 receptor (GLP-1R).{66609} It induces cAMP accumulation in HEK293 cells expressing human GLP-1R (EC50 = 3.05 nM) and is selective for GLP-1R over the glucagon receptor (GCGR), gastric inhibitory polypeptide (GIP) receptor, and GLP-2R at 100 nM. Orforglipron (0.1, 1, or 10 mg/kg) prevents increases in blood glucose levels in glucose-injected fasted mice expressing human GLP-1R but not in glucose-injected Glp1r-/- fasted mice. In vivo, orforglipron (5.4 mg/kg) decreases blood glucose and serum insulin levels in glucose-injected cynomolgus monkeys. It reduces mean food intake in cynomolgus monkeys when administered at doses of 0.05 or 0.1 mg/kg per day.
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