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525143

Sigma-Aldrich

cPLA2α Inhibitor - Calbiochem

cPLA2α Inhibitor is a cell-permeable, highly specific and potent inhibitor of cPLA2α (cytosolic phospholipase A2α) (IC50 = 1.8 nM).

Synonym(s):

cPLA2α Inhibitor - Calbiochem, N-{(2S,4R)-4-(Biphenyl-2-ylmethyl-isobutyl-amino)-1-[2-(2,4-difluorobenzoyl)-benzoyl]-pyrrolidin-2-ylmethyl}-3-[4-(2,4-dioxothiazolidin-5-ylidenemethyl)-phenyl]acrylamide, HCl, cPLA2α Inhibitor

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About This Item

Empirical Formula (Hill Notation):
C49H44F2N4O5S
Molecular Weight:
838.96
UNSPSC Code:
12352200

Quality Level

100

Assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

off-white

solubility

DMSO: 2 mg/mL
75% acetic acid: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

General description

This product has been discontinued.



A cell-permeable 1,2,4-trisubstituted pyrrolidine derivative that acts as a highly specific and potent inhibitor of cPLA2α (cytosolic phospholipase A2α) (IC50 = 1.8 nM). Blocks the release of eicosanoids from A23187-stimulated THP-1 cells (IC50 = 22 nM for arachidonic acid, 31 nM for prostaglandin E2, 13 nM for leukotriene C4). Displays over 230-fold greater potency in the enzyme assay and ~ 3900-fold greater potency in the cellular assay than AACOCF3 (Cat. No. 100109). Does not exert any significant effects on the activities of cycloxygenase and 5-lipoxygenase.

A cell-permeable, highly specific, potent inhibitor of cytosolic phospholipase A2α (cPLA2α) (IC50 = 1.8 nM). Blocks the release of eicosanoids from A23187-stimulated THP-1 cells (IC50 = 22 nM for arachidonic acid; 31 nM for prostaglandin E2; 13 nM for leukotriene C4). Exhibits ~230-fold greater potency in enzyme assays and ~3900-fold greater potency in cellular assays compared to AACOCF3 (Cat. No. 100109). Does not significantly affect the activities of cyclooxygenase and 5-lipoxygenase.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
cPLA2α
Product does not compete with ATP.
Reversible: no
Target IC50: 1.8 nM against cPLA2α (cytosolic phospholipase A2α

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Seno, K., et al. 2000. J. Med. Chem.43, 1041.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

10-13 - German Storage Class 10 to 13

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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