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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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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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Overview

Key Spec Table

CAS #Empirical Formula
955272-06-7C₁₉H₁₅ClN₄O₂

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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 to brown solid
      Hill FormulaC₁₉H₁₅ClN₄O₂
      Chemical formulaC₁₉H₁₅ClN₄O₂
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetNOX1- and NOX4-containing NADPH oxidase activity
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.34032.0001 04055977281767