1. GPCR/G Protein
  2. Glucagon Receptor
  3. Cotadutide acetate

Cotadutide acetate (Synonyms: MEDI0382 acetate)

Cat. No.: HY-P2231A Purity: 96.67%
Handling Instructions

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.

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Cotadutide acetate Chemical Structure

Cotadutide acetate Chemical Structure

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5 mg USD 980 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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].

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].

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
Molecular Weight

3788.14

Formula

C₁₆₉H₂₅₆N₄₂O₅₇

Sequence

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)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (0.53 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

References

Purity: 96.67%

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Keywords:

CotadutideMEDI0382MEDI 0382MEDI-0382Glucagon ReceptorGCGRFOODuptakediabeteT2D obesityInhibitorinhibitorinhibit

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Cotadutide acetate
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