525143 | cPLA2α Inhibitor - Calbiochem

525143
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₄₉H₄₄F₂N₄O₅S

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      525143-500UG
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          Plastic ampoule 500 μg
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          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 -20°C
          Hygroscopic
          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
          ReferencesSeno, K., et al. 2000. J. Med. Chem. 43, 1041.