Cotadutide (MEDI0382) acetate 是一种有效的胰高血糖素样肽-1 (GLP-1) 和胰高血糖素受体 (GCGR) 双重激动剂，EC₅₀ 值分别为 6.9 pM 和 10.2 pM。Cotadutide acetate 可促进减肥，控制血糖，以及减轻纤维化。Cotadutide acetate 可用于肥胖和 2 型糖尿病 (T2D) 的研究。

Cotadutide (MEDI0382) acetate is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC 50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide acetate can be used in the research of obesity and type 2 diabetes (T2D).

Solid

EC50: 6.9 pM (GLP-1); 10.2 pM (GCGR)

Cotadutide acetate 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) acetate 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) acetate induces mitochondrial turnover and enhances mitochondrial function in mouse primary hepatocytes.
has not independently confirmed the accuracy of these methods. They are for reference only.

Cotadutide (10?nmol/kg, s.c., once) acetate 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) acetate reduces body weight in DIO mice.
Cotadutide (30 nmol/kg, s.c., once a day for 6 weeks) acetate reduces hepatic fibrosis and inflammation in in ob/ob AMLN NASH mice.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisturePowder -80°C 2 years；-20°C 1 year

1-{palmtoyl-Glu}; HSQGTFTSDKSEYLDSERARDFVAWLEAGG (Amide bridge: Glu1-Lys10)

1-{palmtoyl-Glu}; His-Ser-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Lys-Ser-Glu-Tyr-Leu-Asp-Ser-Glu-Arg-Ala-Arg-Asp-Phe-Val-Ala-Trp-Leu-Glu-Ala-Gly-Gly (Amide bridge: Glu1-Lys10)

[1]. Henderson SJ,et al. Robust anti-obesity and metabolic effects of a dual GLP-1/glucagon receptor peptide agonist in rodents and non-human primates.Diabetes Obes Metab. 2016 Dec;18(12):1176-1190.
[2]. Resolution of NASH and hepatic fibrosis by the GLP-1R/GcgR dual-agonist Cotadutide via modulating mitochondrial function and lipogenesis. Nat Metab. 2020 May;2(5):413-431.

In Vitro: DMSO : 12.5 mg/mL (3.30 mM; Need ultrasonic)H₂O : 2 mg/mL (0.53 mM; Need ultrasonic)配制储备液