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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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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
955272-06-7C₁₉H₁₅ClN₄O₂

Products

Catalog NumberPackaging Qty/Pack
5.34032.0001 Glass bottle 10 mg
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
Catalog Number GTIN
5.34032.0001 04055977281767

Documentation

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

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.