Cotadutide acetate(Synonyms: MEDI0382 acetate)

Cotadutide acetate;(Synonyms: MEDI0382 acetate) 纯度: 98.01%

Cotadutide acetate (MEDI0382 acetate) 是胰高血糖素样肽-1 (GLP-1) 和胰高血糖素受体 (glucagon receptor) 的有效双重肽激动剂,EC50 值分别为 6.9 pM 和 10.2 pM。Cotadutide acetate (MEDI0382 acetate) 有促进减肥和控制血糖的能力,有潜力用于肥胖症和 2 型糖尿病 (T2D) 的研究。

Cotadutide acetateamp;;(Synonyms: MEDI0382 acetate)

Cotadutide acetate Chemical Structure

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Cotadutide acetate (MEDI0382 acetate) is a potent peptide dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate (MEDI0382 acetate) exhibits ability to facilitate both weight loss and glycaemic control, has the potential for obesity and type 2 diabetes (T2D) treatment[1].

IC50 Target

EC50: 6.9 pM (GLP-1); 10.2 pM (glucagon receptor)[1]

(In Vitro)

Cotadutide acetate (MEDI0382 acetate) shows EC50 values of 6.9 and 10.2 pM as measured by cAMP generation in CHO cells over‐expressing human recombinant GLP‐1 or glucagon receptors in the presence of 0.1% BSA, which are within 10‐fold of the native ligands[1].
Cotadutide acetate (MEDI0382 acetate) stimulates a concentration‐dependent increase in cAMP accumulation in rat (INS‐1 832/3) and human (EndoC‐βH1) pancreatic β‐cell lines (EC50=226 pM, 1051 pM, respectively ), as well as rat, mouse and human hepatocytes (462 pM, 840 pM, 1447 pM, respectively)[1].
Cotadutide acetate (MEDI0382 acetate) has relative potency against GLP‐1R and GCGR activity in human, cynomolgus monkey, mouse and rat transfected GLP‐1 (GLP‐1R) or glucagon (GCGR) receptors expressed CHO cells, The EC50 values are 188 pM, 682 pM; 5.2 pM, 318 pM; 74 pM, 614 pM; and 50 pM, 24173 pM for Human, monkey, mouse and rat GLP‐1R and GCGR activities, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

(In Vivo)

Cotadutide acetate (MEDI0382 acetate) (subcutaneous injection; 10 nmol/kg; once) robustly suppresses food intake in DIO mice relative to vehicle‐treated controls during 0‐12 hours after administration. Mean food intake is reduced during this time interval to approximately 31% of control mice treated with vehicle. The effect of MEDI0382 is evident early (0‐2 hours postdose), the terminal plasma half‐life of MEDI0382 in mice after subcutaneous administration is approximately 5 hours[1].
Cotadutide acetate (MEDI0382 acetate) (subcutaneous injection; 10 or 30 nmol/kg; once daily; 14-16 weeks) reduces body weight. reduced body weight.The mean body weight of vehicle‐treated animals increased by 2.5% of starting body weight over the course of the 4‐week study, whereas the mean body weight loss is 21%, 30% of starting body weight at dose levels of 10 nmol/kg MEDI0382, 30 nmol/kg MEDI0382, respectively [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: DIO mice[1]
Dosage: 10 nmol/kg
Administration: Subcutaneous injection
Result: Showed a redction of food intake in mice after an acute administration.
Animal Model: DIO mice[1]
Dosage: 10 or 30 nmol/kg
Administration: Subcutaneous injection
Result: Reduced body weight and food intake and improves glucose tolerance in DIO mice.

Clinical Trial






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)

Sequence Shortening

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


Room temperature in continental US; may vary elsewhere.


Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

In Vitro:;

DMSO : 12.5 mg/mL (3.30 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.2640 mL 1.3199 mL 2.6398 mL
5 mM
10 mM


储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百

  • 1.

    请依序添加每种溶剂:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: 1.25 mg/mL (0.33 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.25 mg/mL (0.33 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: 1.25 mg/mL (0.33 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.25 mg/mL (0.33 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: ≥ 1.25 mg/mL (0.33 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (0.33 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
  • [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.