5.34032
NOX Inhibitor IV, GKT136901
Synonim(y):
NOX Inhibitor IV, GKT136901, 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
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Informacje o tej pozycji
Wzór empiryczny (zapis Hilla):
C19H15ClN4O2
Numer CAS:
Masa cząsteczkowa:
366.80
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
eCl@ss:
32160701
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Pomoc techniczna
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Pozwól nam pomócassay
≥98% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow to brown
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
SMILES string
Clc1c(cccc1)[n]2[nH]c3c([c]2=O)c([n]([c](c3)=O)Cc4ncccc4)C
InChI
1S/C19H15ClN4O2/c1-12-18-15(10-17(25)23(12)11-13-6-4-5-9-21-13)22-24(19(18)26)16-8-3-2-7-14(16)20/h2-10,22H,11H2,1H3
InChI key
DNKYHHFCPXKFIY-UHFFFAOYSA-N
General description
An 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.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
NOX1- and NOX4-containing NADPH oxidase activity
NOX1- and NOX4-containing NADPH oxidase activity
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.
Other Notes
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.
Laleu, B., et al. 2010. J. Med. Chem.53, 7715.
Sedeek, M., et al. 2010. Am. J. Physiol. Renal Physiol.299, F1348.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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Klasa składowania
11 - Combustible Solids
WGK
WGK 3
Temperatura zapłonu (°F)
Not applicable
Temperatura zapłonu (°C)
Not applicable
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