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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: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: 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
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      Übersicht

      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
      Bestellnummer GTIN
      525143 0

      Documentation

      cPLA2α Inhibitor - Calbiochem Analysenzertifikate

      TitelChargennummer
      525143

      Literatur

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

      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.