A potent gastrin/CCKB receptor antagonist
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AG-041R

Item No. 10010129

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $76

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    5 mg

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    10 mg

    $646

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    50 mg

    $2,088

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    Cayman Chemical
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    Product Description

    AG-041R is a potent gastrin/CCK2 receptor antagonist that exhibits selective binding for CCK2 compared to CCK1.1 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.1,2 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.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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(3-4), 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(2), 530-536 (1999).

    3. Sun, W.H., Zhu, F., Chen, G.S., 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(2), 302-311 (2008).