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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.

NOX Inhibitor IV, GKT136901 - CAS 955272-06-7 - Calbiochem 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
534032
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Tabulka spec. kláve

CAS #Empirical Formula
955272-06-7C₁₉H₁₅ClN₄O₂

Products

Katalogové čísloBalení ks/bal.
5.34032.0001 Skleněná láhev 10 mg
Přidat k oblíbeným položkám
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
Katalogové číslo GTIN
5.34032.0001 04055977281767