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AG-041R Exclusive

Cayman Chemical Item Number 10010129

(CAS 199800-49-2)

AG-041R (CAS 199800-49-2)

See more	Receptor Antagonist (45) Apoptosis (183) Cancer (606)

Description

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., and 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).

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	199800-49-2
Molecular Formula	C₃₁H₃₆N₄O₅
Formula Weight	544.7
Formulation	A crystalline solid
Purity	≥98%
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard CCOC(OCC)CN1c2ccccc2C(CC(=O)Nc2ccc(C)cc2)(NC(=O)Nc2ccc(C)cc2)C1=O

Background Reading

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).

Lindström, E., Björkqvist, M., and Håkanson, R. Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells. Br J Pharmacol 127 530-536 (1999).

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).

Size	Price	Quantity	Subtotal
1 mg	$36.00		$0.00
5 mg	$162.00		$0.00
10 mg	$288.00		$0.00
50 mg	$1,260.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-12. Prices are subject to change without notice.

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Related Products

NS-398

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