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530538 cPLA2α Inhibitor II, Pyrrophenone - CAS 341973-06-6 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
341973-06-6C₄₉H₃₇F₂N₃O₅S₂

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      Description
      OverviewA 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.
      Catalogue Number530538
      Brand Family Calbiochem®
      SynonymsPhospholipase A2α Inhibitor
      References
      ReferencesOno, T., et al. 2002. Biochem. J. 363, 727.
      Seno, K., et al. 2001. Bioorg. Med. Chem. Lett. 11, 587.
      Product Information
      CAS number341973-06-6
      FormOff-white powder
      Hill FormulaC₄₉H₃₇F₂N₃O₅S₂
      Chemical formulaC₄₉H₃₇F₂N₃O₅S₂
      Quality LevelMQ100
      Biological Information
      Primary TargetPLA2a
      Primary Target IC<sub>50</sub>4.2 nM
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.30538.0001 04055977260892