150379-37-6
Chemical Structure
CGP-43182
- CAS No.: 150379-37-6
- Formula:C16H15Cl2NO5
- Molecular Weight:372.20
IUPAC Name: N-(2,3-dichlorophenyl)-2-hydroxy-4-oxo-1,5-dioxaspiro[5.5]undec-2-ene-3-carboxamide
InChIKey: KSXVYLXVMKLSOE-UHFFFAOYSA-N
SMILES: O=C(NC1=CC=CC(Cl)=C1Cl)C2=C(OC3(OC2=O)CCCCC3)O
Biological Activity: CGP-43182 is a secretory phospholipase A2 group II (sPLA2) inhibitor with an IC50 of 2.8 μM. CGP-43182 binds to the active site of the enzyme, blocks IL1β-stimulated gene expression and NFκB activation, and inhibits the production of prostaglandin and nitric oxide (NO). CGP-43182 exhibits anti-inflammatory activity in multiple inflammatory models and can be used for studies on adjuvant arthritis, carrageenan-induced edema, pertussis pleurisy, and glomerular inflammatory responses[1][2][3][4].
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CGP-43182 | CGP-43182 is a secretory phospholipase A2 group II (sPLA2) inhibitor with an IC50 of 2.8 μM. CGP-43182 binds to the active site of the enzyme, blocks IL1β-stimulated gene expression and NFκB activation, and inhibits the production of prostaglandin and nitric oxide (NO). CGP-43182 exhibits anti-inflammatory activity in multiple inflammatory models and can be used for studies on adjuvant arthritis, carrageenan-induced edema, pertussis pleurisy, and glomerular inflammatory responses. | |||||||||||||||||||||
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References
- [1]. Scholz-Pedretti K, et al. Inhibition of NFkappaB-mediated pro-inflammatory gene expression in rat mesangial cells by the enolized 1,3-dioxane-4, 6-dione-5-carboxamide, CGP-43182. British journal of pharmacology. 2000 Jul;130(5):1183-90.
- [2]. Pfeilschifter J, et al. Cytokine-stimulated secretion of group II phospholipase A2 by rat mesangial cells. Its contribution to arachidonic acid release and prostaglandin synthesis by cultured rat glomerular cells. J Clin Invest. 1993 Nov;92(5):2516-23.
- [3]. Pfeilschifter J, et al. Contribution of group II phospholipase A2 to arachidonic acid release and prostaglandin synthesis by mesangial cells[J]. Agents and Actions, 1994, 41(Suppl 2): C150-C152.
- [4]. Rosenstock M, et al. Dual regulation of PLA2 and PGI2 production by G proteins in bovine aortic endothelial cells. The American journal of physiology. 1996 Aug;271(2 Pt 1):C555-62.
