10010129  AG-041R

(CAS 199800-49-2)



• See below for pricing and ordering
• See more Receptor Antagonist; Apoptosis; Cancer

For active pharmaceutical ingredients (APIs) related to AG-041R, see Cayman Pharma

The peptide hormone gastrin acts through G protein-coupled cholecystokinin-2 (CCKB) 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/CCKB receptor antagonist that exhibits selective binding for CCKB compared to CCKA.1 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.2,1 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 (Catalog No. 70590) at 10 µM.3
1  Chiba, T., Kinoshita, Y., Sawada, M., et al. The role of endogenous gastrin in the development of enterochromaffin-like cell carcinoid tumors in Mastomys natalensis: A study with the specific gastrin receptor antagonist AG-041R. Yale J Biol Med 71 247-255 (1998).
2  Lindström, E., Björkqvist, M., Håkanson, R. Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells. Br J Pharmacol 127 530-536 (1999).
3  Sun, W., Zhu, F., Chen, G., et al. Blockade of cholecystokinin-2 receptor and cyclooxygenase-2 synergistically induces cell apoptosis, and inhibits the proliferation of human gastric cancer cells in vitro. Cancer Lett 263 302-311 (2008).

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Pricing Information

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Size Price Quantity
1 mg €42.00
5 mg €190.00
10 mg €336.00
50 mg €1,470.00
Pricing updated 2010-08-01.
Prices are subject to change without notice.

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