530538 cPLA2α Inhibitor II, Pyrrophenone - Calbiochem

530538
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₄₉H₃₇F₂N₃O₅S₂

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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
      FormOff-white powder
      Hill FormulaC₄₉H₃₇F₂N₃O₅S₂
      Chemical formulaC₄₉H₃₇F₂N₃O₅S₂
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPLA2a
      Primary Target IC<sub>50</sub>4.2 nM
      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 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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      cPLA2α Inhibitor II, Pyrrophenone - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Ono, T., et al. 2002. Biochem. J. 363, 727.
      Seno, K., et al. 2001. Bioorg. Med. Chem. Lett. 11, 587.

      Brochure

      Title
      NPI Flyer- Epigenetics and Nuclear Function Feature
      New Products - Antibodies, Small Molecule, Inhibitors (MM)

      Technical Info

      Title
      White Paper: Further considerations of antibody validation and usage.
      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.

      Revision31-October-2014 JSW
      SynonymsPhospholipase A2α Inhibitor
      DescriptionA 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.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₄₉H₃₇F₂N₃O₅S₂
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage -20°C
      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.
      Toxicity Standard Handling
      ReferencesOno, T., et al. 2002. Biochem. J. 363, 727.
      Seno, K., et al. 2001. Bioorg. Med. Chem. Lett. 11, 587.