AG-041R

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. 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. 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 (Cay-70590) at 10 µM.Formal Name: (3R)-1-(2,2-diethoxyethyl)-2,3-dihydro-N-(4-methylphenyl)-3-[[[(4-methylphenyl)amino]carbonyl]amino]-2-oxo-1H-indole-3-acetamide. CAS Number: 159883-95-1. Molecular Formula: C31H36N4O5. Formula Weight: 544.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMSO: 10 mg/ml, Ethanol: 5 mg/ml. lambdamax: 247 nm. SMILES: CC1=CC=C(NC(N[C@@]2(C3=C(C=CC=C3)N(CC(OCC)OCC)C2=O)CC(NC4=CC=C(C)C=C4)=O)=O)C=C1. InChi Code: InChI=1S/C31H36N4O5/c1-5-39-28(40-6-2)20-35-26-10-8-7-9-25(26)31(29(35)37,19-27(36)32-23-15-11-21(3)12-16-23)34-30(38)33-24-17-13-22(4)14-18-24/h7-18,28H,5-6,19-20H2,1-4H3,(H,32,36)(H2,33,34,38)/t31-/m1/s1. InChi Key: KOLPMNSDISYEBU-WJOKGBTCSA-N.