5.30538
cPLA2α Inhibitor II, Pyrrophenone
Synonym(s):
cPLA2α Inhibitor II, Pyrrophenone, Phospholipase A2α Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C49H37F2N3O5S2
CAS Number:
Molecular Weight:
849.96
UNSPSC Code:
12352200
NACRES:
NA.77
Assay
≥98% (HPLC)
Quality Level
form
powder
potency
4.2 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 100 mg/mL
storage temp.
−20°C
General description
Pyrrophenone is a cell-permeable, non-toxic, pyrolidine derivative that acts as a highly potent, and reversible inhibitor of cytosolic phospholipase A2a (cPLA2a; IC50 = 4.2 nM). Does not inhibit the activities of PLA IB and IIA groups even at higher concentrations (~250 µM). Unlike AACOCF3 (Cat. No. 100109), its action is shown to be rapid and does not require a pre-incubation period. Diminishes the release of arachidonic acid (IC50 = 24 nM), prostaglandin E2 (PGE2; IC50 = 25 nM) and leukotriene C4 (IC50 = 14 nM) in A23187 stimulated THP-1 cells. Its effects on production of PGE2 and thromboxane B2 are comparable to those of indomethacin. Also shown to inhibit the lysophospholipase and esterase activity of cPLA2&alpha.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PLA2a
PLA2a
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Other Notes
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Certificates of Analysis (COA)
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