产品描述:
The peptide hormone gastrin acts through G protein-coupled cholecystokinin-2 (CCK2) 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/CCK2 receptor antagonist that exhibits selective binding for CCK2 compared to CCK1.{16543} AG-041R inhibits gastrin-evoked secretion of pancreastatin (IC50 = 2.2 nM) as well as gastrin-induced histamine release and cell growth of Mastomys ECL carcinoid tumor cells.{16543,16568} 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 (Item No. 70590) at 10 µM.{16544}