533371 Acid Ceramidase Inhibitor IV, BOC - Calbiochem

533371
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₄H₂₁FN₂O₃

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      5.33371.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, chemically and metabolically stable (t1/2 >5 h in aqueous buffers at pH 4.5 and 7.4; t1/2 >2 h in murine plasma at 37 °C) benzoxazolone carboxamide (BOC) compound that inhibits acid ceramidase (AC) activity in a potent (IC50 = 79 nM against HEK293 lysosomal lysate AC activity) and selective manner via covalent modification of the active site Cys143, exhibiting little or no potency toward a panel of 15 enzymes, including proteases, lipoxygenases, cyclooxygenases, sPLA2, and monoacylglycerol lipase (67% inhibition of cathepsin D and ≤17.1% inhibition of the rest at 10 µM). Culture treatment results in long-lasting (>6 h) suppression of cellular AC activity in murine macrophage-like Raw 264.7 and human colon adenocarcinoma SW403 cells (IC50 with 3 h treatment = 400 and 825 nM, respectively), as well as built-ups of cellular AC substrates Cer(d18:0/16:0) & Cer(d18:1/16:0) in a dose-dependent manner. Intraperitoneal injection (10 mg/kg) effectively inhibits tissue AC activity in multiple organs, including lung, heart, kidney, brain hippocampus, and liver (by 70%, 60%, 44%, 40%, 35%, respectively), with good pharmacokinetic properties (Tmax = 30 min, Cmax = 1.768 µg/mL, t1/2 = 458 min, AUC0-8 h = 0.31 mg·min/mL; 10 mg/kg i.p.).

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number533371
          Brand Family Calbiochem®
          SynonymsAC Inhibitor IV
          References
          ReferencesPizzirani, D., et al. 2015. Angew. Chem. Int. Ed. Engl. 54, 485.
          Product Information
          FormOff-white solid
          Hill FormulaC₂₄H₂₁FN₂O₃
          Chemical formulaC₂₄H₂₁FN₂O₃
          ReversibleN
          Applications
          Biological Information
          Primary TargetAcid ceramidase
          Primary Target IC<sub>50</sub>79 nM against HEK293 lysosomal lysate AC activity
          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 +2°C to +8°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

          Acid Ceramidase Inhibitor IV, BOC - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Pizzirani, D., et al. 2015. Angew. Chem. Int. Ed. Engl. 54, 485.
          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.

          Revision20-November-2015 JSW
          SynonymsAC Inhibitor IV
          DescriptionA cell-permeable, chemically and metabolically stable (t1/2 >5 h in aqueous buffers at pH 4.5 and 7.4; t1/2 >2 h in murine plasma at 37 °C) benzoxazolone carboxamide (BOC) compound that inhibits acid ceramidase (AC) activity in a potent (IC50 = 79 nM against HEK293 lysosomal lysate AC activity) and selective manner via covalent modification of the active site Cys143, exhibiting little or no potency toward a panel of 15 enzymes, including proteases, lipoxygenases, cyclooxygenases, sPLA2, and monoacylglycerol lipase (67% inhibition of cathepsin D and ≤17.1% inhibition of the rest at 10 µM). Culture treatment results in long-lasting (>6 h) suppression of cellular AC activity in murine macrophage-like Raw 264.7 and human colon adenocarcinoma SW403 cells (IC50 with 3 h treatment = 400 and 825 nM, respectively), as well as built-ups of cellular AC substrates Cer(d18:0/16:0) & Cer(d18:1/16:0) in a dose-dependent manner. Intraperitoneal injection (10 mg/kg) effectively inhibits tissue AC activity in multiple organs, including lung, heart, kidney, brain hippocampus, and liver (by 70%, 60%, 44%, 40%, 35%, respectively), with good pharmacokinetic properties (Tmax = 30 min, Cmax = 1.768 µg/mL, t1/2 = 458 min, AUC0-8 h = 0.31 mg·min/mL; 10 mg/kg i.p.).
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₄H₂₁FN₂O₃
          Purity≥98% by HPLC
          SolubilityDMSO (40 mg/ml)
          Storage +2°C to +8°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
          ReferencesPizzirani, D., et al. 2015. Angew. Chem. Int. Ed. Engl. 54, 485.