530538 cPLA2α Inhibitor II, Pyrrophenone - Calbiochem

530538
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₄₉H₃₇F₂N₃O₅S₂

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30538.0001
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          Glass bottle 1 mg
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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
          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.
          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.