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.