Sigma-Aldrich Cpla2a Inhibitor Ii Pyrrop

Assay

≥98% (HPLC)

Quality Level

100

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

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.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.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
PLA2a

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Ono, T., et Al. 2002.Biochem. J. 363,727.
Seno, K., et Al. 2001.Bioorg. Med. Chem. Lett. 11,587.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany