A potent CCK2/gastrin receptor antagonist that exhibits selective binding for CCK2 compared to CCK1; 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

AG-041R – 5 mg

Brand:
Cayman
CAS:
159883-95-1
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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SKU: 10010129 - 5 mg Category:

Description

A potent CCK2/gastrin receptor antagonist that exhibits selective binding for CCK2 compared to CCK1; 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

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

Synonyms: 

Molecular weight: 544.7

CAS: 159883-95-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors

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