CGP 43182 - CAS 150379-37-6
Catalog number: 150379-37-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C16H15Cl2NO5
Molecular Weight:
372.20
COA:
Inquire
Targets:
Others
Description:
CGP 43182, a dioxaspiro compound, has been found to a IIA sPLA2 inhibitor that could have potential anti-inflammatory effect and also in influencing the synergistic effect brought by pro-inflammatory genes.
Purity:
98%
Appearance:
Powder
Synonyms:
Cgp 43182; Cgp-43182; Cgp43182. N-(2,3-Dichlorophenyl)-2-hydroxy-4-oxo-1,5-dioxaspiro(5.5)undec-2-ene-3-carboxamide; N-(2,3-dichlorophenyl)-2-hydroxy-4-oxo-1,5-dioxaspiro[5.5]undec-2-ene-3-carboxamide; AC1L2SHN; DTXSID00164535
Storage:
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
MSDS:
Inquire
Quality Standard:
In-house standard
Quantity:
Milligram-Grams
InChIKey:
KSXVYLXVMKLSOE-UHFFFAOYSA-N
InChI:
InChI=1S/C16H15Cl2NO5/c17-9-5-4-6-10(12(9)18)19-13(20)11-14(21)23-16(24-15(11)22)7-2-1-3-8-16/h4-6,21H,1-3,7-8H2,(H,19,20)
Canonical SMILES:
C1CCC2(CC1)OC(=C(C(=O)O2)C(=O)NC3=C(C(=CC=C3)Cl)Cl)O
1.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.
Pfeilschifter J;Schalkwijk C;Briner VA;van den Bosch H J Clin Invest. 1993 Nov;92(5):2516-23.
Potent pro-inflammatory cytokines, such as interleukin 1 (IL-1) or tumor necrosis factor (TNF) alpha have been found to increase group II phospholipase A2 (PLA2) synthesis and secretion by mesangial cells. In all cases 85-90% of the enzyme is secreted from the cells and a parallel increase in prostaglandin (PG)E2 synthesis is observed. We report here that co-incubation with a monoclonal antibody that specifically binds and neutralizes rat group II PLA2 attenuates IL-1 beta and TNF alpha-stimulated PGE2 production by 45% and 52%, respectively. CGP43182, a specific inhibitor of group II PLA2, potently blocks mesangial cell group II PLA2 in vitro with a half-maximal inhibitory concentration (IC50) of 1.5 microM, while only slightly affecting mesangial cell high molecular weight PLA2. CGP 43182 markedly attenuates IL-1 beta- and TNF alpha-stimulated PGE2 synthesis in intact mesangial cells with IC50's of 1.3 and 1.0 microM, respectively. PLA2 secreted from cytokine-stimulated mesangial cells was purified to homogeneity. Addition of the purified enzyme to unstimulated mesangial cells causes a marked release of arachidonic acid and a subsequent increased synthesis of PGE2. Moreover, addition of purified PLA2 to a cloned rat glomerular epithelial cell line and cultured bovine glomerular endothelial cells augmented both arachidonic acid release and PGE2 synthesis, with the endothelial cells being especially sensitive.
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