Description

Mazdutide (IBI-362; LY-3305677) TFA is a long-acting synthetic oxyntomodulin analog. Mazdutide is also a co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR). Mazdutide TFA binds human and mouse GCGR (Ki: 17.7 nM and 15.9 nM, respectively) and GLP-1R (Ki: 28.6 nM and 25.1 nM, respectively) and stimulates insulin secretion from mouse islets (EC50: 5.2 nM). Mazdutide TFA is used in studies of obesity and type 2 diabetes (T2D)[1][2][3].—Metabolism-protein/nucleotide metabolism–C210H322N46O67.xC2HF3O2—-[1]Chen T, et al. The Design and Optimization of Monomeric Multitarget Peptides for the Treatment of Multifactorial Diseases. J Med Chem. 2022 Mar 10;65(5):3685-3705.|[2]Jiang H, et al. A phase 1b randomised controlled trial of a glucagon-like peptide-1 and glucagon receptor dual agonist IBI362 (LY3305677) in Chinese patients with type 2 diabetes. Nat Commun. 2022 Jun 24;13(1):3613.|[3]Chen Y, Mezo A, Coskun T, et al. 682-P: novel dual glucagon and glucagon-like peptide-1 receptor agonist LY3305677 improves glucose control, reduces body weight, and increases energy expenditure in mice[J]. Diabetes, 2021, 70(Supplement_1).—-4563.06 (free base)—-[Mazdutide (TFA)]–Metabolic Disease–10 mM in DMSO–GCGR;GLP Receptor—-GPCR/G Protein–Peptides