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525143 cPLA2α Inhibitor - Calbiochem

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

cPLA2α Inhibitor - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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

Primary Target: cPLA2α
525143
  
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₄₉H₄₄F₂N₄O₅S
Description
Overview

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.
Catalogue Number525143
Brand Family Calbiochem®
SynonymsN-{(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
References
ReferencesSeno, K., et al. 2000. J. Med. Chem. 43, 1041.
Product Information
ATP CompetitiveN
FormOff-white solid
Hill FormulaC₄₉H₄₄F₂N₄O₅S
Chemical formulaC₄₉H₄₄F₂N₄O₅S
Hygroscopic Hygroscopic
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationcPLA2α Inhibitor is a cell-permeable, highly specific and potent inhibitor of cPLA2α (cytosolic phospholipase A2α) (IC50 = 1.8 nM).
Biological Information
Primary TargetcPLA2α
Primary Target IC<sub>50</sub>1.8 nM against cPLA2α (cytosolic phospholipase A2α
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
525143 0

Documentation

cPLA2α Inhibitor - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

cPLA2α Inhibitor - Calbiochem Certificates of Analysis

TitleLot Number
525143

References

Reference overview
Seno, K., et al. 2000. J. Med. Chem. 43, 1041.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision27-September-2010 RFH
SynonymsN-{(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
DescriptionA 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.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₄₉H₄₄F₂N₄O₅S
Structure formulaStructure formula
Purity≥98% by HPLC
Solubility75% aqueous acetic acid (5 mg/ml) or DMSO (2 mg/ml)
Storage Protect from light
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesSeno, K., et al. 2000. J. Med. Chem. 43, 1041.