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编 号:F746697
分子式:C167H252N42O55
分子量:3728.09
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生物活性:
Cotadutide (MEDI0382) is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide can be used in the research of obesity and type 2 diabetes (T2D).

体内研究:
Cotadutide (10?nmol/kg, s.c., once) suppresses food intake in DIO mice relative to vehicle‐treated controls.Cotadutide (10 or 30?nmol/kg, s.c., once daily for 14-16 weeks) reduces body weight in DIO mice.Cotadutide (30 nmol/kg, s.c., once a day for 6 weeks) reduces hepatic fibrosis and inflammation in in ob/ob AMLN NASH mice.Animal Model:Diet-induced obesity (DIO) mice
Dosage:10?nmol/kg
Administration:Subcutaneousinjection (s.c.)
Result:Showed a redction of food intake in mice after an acute administration.
Animal Model:Diet-induced obesity (DIO) mice
Dosage:10 or 30?nmol/kg
Administration:Subcutaneousinjection (s.c.)
Result:Reduced body weight and food intake, and improved glucose tolerance in DIO mice.

体外研究:
Cotadutide stimulates a concentration-dependent increase in cAMP accumulation in rat (INS-1 832/3) and human (EndoC-βH1) β-cell lines (EC50: 226 pM and 1051 pM, respectively?), as well as rat, mouse and human hepatocytes (EC50: 462 pM, 840 pM, 1447 pM, respectively).Cotadutide (100 pM-1 μM) potentiates glucose-stimulated insulin secretion in the rat (INS-1 832/3) pancreatic β‐cell line and increases glucose output in rat hepatocytes.Cotadutide (100 nM, 2 h) induces mitochondrial turnover and enhances mitochondrial function in mouse primary hepatocytes.
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