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

Potent, orally available dual inhibitor of NOX1/NOX4. Blocks NOX-mediated ROS outburst and efficiently scavenges peroxynitrite.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 2-(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

Primary Target: NOX1- and NOX4-containing NADPH oxidase activity
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534032
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CAS #Empirical Formula
955272-06-7C₁₉H₁₅ClN₄O₂

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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 to brown solid
      Hill FormulaC₁₉H₁₅ClN₄O₂
      Chemical formulaC₁₉H₁₅ClN₄O₂
      ReversibleY
      Quality LevelMQ100
      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
      Global Trade Item Number
      Référence GTIN
      5.34032.0001 04055977281767

      Documentation

      NOX Inhibitor IV, GKT136901 - CAS 955272-06-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      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.
      Fiche technique

      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.

      Revision22-July-2024 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 to brown 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 Protect from light
      +2°C to +8°C
      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.