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534032 | NOX Inhibitor IV, GKT136901 - CAS 955272-06-7 - Calbiochem

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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₉H₁₅ClN₄O₂ 955272-06-7

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      5.34032.0001
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          Glass bottle 10 mg
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          Description
          OverviewAn orally bioavailable, non-toxic pyrazolopyridinedione based compound that acts as a potent and reversible inhibitor of NOX1- and NOX4-containing NADPH oxidase activity (Ki = 160 and 165 nM, respectively, Amplex Red assay) and devoid of antioxidant properties. At higher concentrations, affects NOX2 (Ki = 1.53 uM). Blocks NOX-mediated ROS (reactive oxygen species) outburst in NOX isozyme expressing PMN cell membranes. Exhibits poor affinity towards xanthine oxidase, lipoxygenases-5/12, myeloperoxidase, MAO-B, iNOS and eNOS, several cytochrome P450 isozymes, PTP1B and a panel containing representative ion-channels and kinases at 10 µM. Functions as a selective scavenger of peroxynitrite over nitric oxide, superoxide radical anion and hydroxyl radical.

          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 Number534032
          Brand Family Calbiochem®
          Synonyms2-(2-Chlorophenyl)-4-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo-[4,3-c]pyridine-3,6(2H,5H)-dione, NADPH Oxidase Inhibitor IV, Dual NOX4/NOX1 Inhibitor, GKT-136901
          DescriptionNOX Inhibitor IV, GKT136901
          References
          ReferencesSchildknecht, S., et al. 2014. Curr. Med. Chem. 21, 365.
          Laleu, B., et al. 2010. J. Med. Chem. 53, 7715.
          Sedeek, M., et al. 2010. Am. J. Physiol. Renal Physiol. 299, F1348.
          Product Information
          CAS number955272-06-7
          FormPale yellow solid
          Hill FormulaC₁₉H₁₅ClN₄O₂
          Chemical formulaC₁₉H₁₅ClN₄O₂
          ReversibleY
          Applications
          Biological Information
          Primary TargetNOX1- and NOX4-containing NADPH oxidase 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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Schildknecht, S., et al. 2014. Curr. Med. Chem. 21, 365.
          Laleu, B., et al. 2010. J. Med. Chem. 53, 7715.
          Sedeek, M., et al. 2010. Am. J. Physiol. Renal Physiol. 299, F1348.
          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.

          Revision25-June-2016 JSW
          Synonyms2-(2-Chlorophenyl)-4-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo-[4,3-c]pyridine-3,6(2H,5H)-dione, NADPH Oxidase Inhibitor IV, Dual NOX4/NOX1 Inhibitor, GKT-136901
          DescriptionAn orally bioavailable, non-toxic pyrazolopyridinedione based compound that acts as a potent and reversible inhibitor of NOX1- and NOX4-containing NADPH oxidase activity (Ki = 160 and 165 nM, respectively, Amplex Red assay) and devoid of antioxidant properties. At higher concentrations, affects NOX2 (Ki = 1.53 uM). Blocks NOX-mediated ROS (reactive oxygen species) outburst in NOX isozyme expressing PMN cell membranes. Exhibits poor affinity towards xanthine oxidase, lipoxygenases-5/12, myeloperoxidase, MAO-B, iNOS and eNOS, several cytochrome P450 isozymes, PTP1B and a panel containing representative ion-channels and kinases at 10 µM. Functions as a selective scavenger of peroxynitrite over nitric oxide, superoxide radical anion and hydroxyl radical.
          FormPale yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number955272-06-7
          Chemical formulaC₁₉H₁₅ClN₄O₂
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
          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
          ReferencesSchildknecht, S., et al. 2014. Curr. Med. Chem. 21, 365.
          Laleu, B., et al. 2010. J. Med. Chem. 53, 7715.
          Sedeek, M., et al. 2010. Am. J. Physiol. Renal Physiol. 299, F1348.