Molecular structure of AG-041R, CAS Number: 159883-95-1
AG-041R (CAS 159883-95-1)
Application:
AG-041R is a potent CCK-BR (gastrin/CCKB receptor) antagonist that exhibits selective binding for CCKB compared to CCKA
CAS Number:
159883-95-1
Purity:
≥98%
Molecular Weight:
544.7
Molecular Formula:
C31H36N4O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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Description
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SDS & Certificate of Analysis
AG-041R is a potent CCK-BR (gastrin/cholecystokinin-2 (CCKB) receptor) antagonist that exhibits selective binding for CCKB compared to CCKA. 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 muM) exhibits synergistic inhibitory effects on the cell viability of human gastric cancer cells when administered with the selective COX-2 inhibitor NS-398 at 10 muM.
AG-041R (CAS 159883-95-1) References
- 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. | Chiba, T., et al. 1998. Yale J Biol Med. 71: 247-55. PMID: 10461356
- AG-041R, a novel indoline-2-one derivative, induces systemic cartilage hyperplasia in rats. | Kitamura, H., et al. 2001. Eur J Pharmacol. 418: 225-30. PMID: 11343694
- AG-041R, a gastrin/CCK-B antagonist, stimulates chondrocyte proliferation and metabolism in vitro. | Ochi, M., et al. 2001. Biochem Biophys Res Commun. 283: 1118-23. PMID: 11355888
- AG-041R, a cholecystokinin-B/gastrin receptor antagonist, stimulates the repair of osteochondral defect in rabbit model. | Nakanishi, T., et al. 2002. Eur J Pharmacol. 439: 135-40. PMID: 11937103
- Lansoprazole induces mucosal protection through gastrin receptor-dependent up-regulation of cyclooxygenase-2 in rats. | Tsuji, S., et al. 2002. J Pharmacol Exp Ther. 303: 1301-8. PMID: 12438555
- AG-041R stimulates cartilage matrix synthesis without promoting terminal differentiation in rat articular chondrocytes. | Okazaki, M., et al. 2003. Osteoarthritis Cartilage. 11: 122-32. PMID: 12554128
- Microscopic molecular mobility of amorphous AG-041R measured by solid-state 13C NMR. | Koga, A., et al. 2004. Int J Pharm. 275: 73-83. PMID: 15081139
- AG-041R, a novel indoline-2-one derivative, stimulates chondrogenesis in a bipotent chondroprogenitor cell line CL-1. | Kitamura, H. and Okazaki, M. 2005. Osteoarthritis Cartilage. 13: 287-96. PMID: 15780642
- Efficient asymmetric synthesis of novel gastrin receptor antagonist AG-041R via highly stereoselective alkylation of oxindole enolates. | Emura, T., et al. 2006. J Org Chem. 71: 8559-64. PMID: 17064034
- Blockade of cholecystokinin-2 receptor and cyclooxygenase-2 synergistically induces cell apoptosis, and inhibits the proliferation of human gastric cancer cells in vitro. | Sun, WH., et al. 2008. Cancer Lett. 263: 302-11. PMID: 18258354
- Catalytic asymmetric synthesis of 3-aminooxindoles: enantiofacial selectivity switch in bimetallic vs monometallic Schiff base catalysis. | Mouri, S., et al. 2010. J Am Chem Soc. 132: 1255-7. PMID: 20055386
- Enantioselective synthesis of AG-041R by using N-heteroarenesulfonyl cinchona alkaloid amides as organocatalysts. | Hara, N., et al. 2012. Chemistry. 18: 9276-80. PMID: 22736544
- An organocatalytic Mannich/denitration reaction for the asymmetric synthesis of 3-ethylacetate-substitued 3-amino-2-oxindoles: formal synthesis of AG-041R. | Zhao, K., et al. 2015. Chemistry. 21: 3933-6. PMID: 25630891
- Stereoselective Organocatalytic Synthesis of Oxindoles with Adjacent Tetrasubstituted Stereocenters. | Engl, OD., et al. 2015. Angew Chem Int Ed Engl. 54: 8193-7. PMID: 26033441
- A highly efficient Mukaiyama-Mannich reaction of N-Boc isatin ketimines and other active cyclic ketimines using difluoroenol silyl ethers catalyzed by Ph3PAuOTf. | Yu, JS. and Zhou, J. 2015. Org Biomol Chem. 13: 10968-72. PMID: 26443467
Inhibitor of:
CCK-BR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AG-041R, 1 mg | sc-205202 | 1 mg | $74.00 | |||
AG-041R, 5 mg | sc-205202A | 5 mg | $339.00 |