Cotadutide acetate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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) 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.(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. 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). 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.(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. 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?.

MEDI0382 acetate

Others

Other Targets

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

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3788.1

C169H256N42O57

>98% (HPLC)

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Sequence:1'-{palmtoyl-G}; {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: Ggu1-Lys10)

(-20℃)

With Ice Pack

≥ 2 years