The peptide hormone gastrin acts through G protein-coupled cholecystokinin-2 (CCK) receptors to regulate cell proliferation, differentiation, apoptosis, and gene expression of gastrointestinal cells and exerts trophic effects on a number of gastric cancer cell lines. AG-041R is a potent gastrin/CCK receptor antagonist that exhibits selective binding for CCK compared to CCK AG-041R inhibits gastrin-evoked secretion of pancreastatin (IC = 2.2 nM) as well as gastrin-induced histamine release and cell growth of Mastomys ECL carcinoid tumor cells. AG-041R (1 µM) exhibits synergistic inhibitory effects on the cell viability of human gastric cancer cells when administered in combination with the selective COX-2 inhibitor NS-398 at 10 µM.
AG-041R is a potent and selective CCK2 Receptor/Gastrin antagonist. AG-041R inhibits gastrin-evoked secretion of pancreastatin with an IC50 of 2.2 nM. AG-041R inhibits cell growth of Mastomys ECL carcinoid tumor cells.
分子式
C31H36N4O5
分子量
544.7
CAS号
159883-95-1
运输条件
Room temperature in continental US; may vary elsewhere.