5.34032

NOX Inhibitor IV, GKT136901

• 別名: 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
• 実験式（ヒル表記法）: C₁₉H₁₅ClN₄O₂
• CAS番号: 955272-06-7
• 分子量: 366.80
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: pale yellow to brown
• 溶解性: DMSO: 50 mg/mL
• 保管温度: 2-8°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

詳細

詳細

An orally bioavailable, non-toxic pyrazolopyridinedione based compound that acts as a potent and reversible inhibitor of NOX1- and NOX4-containing NADPH oxidase activity (K_i = 160 and 165 nM, respectively, Amplex Red assay) and devoid of antioxidant properties. At higher concentrations, affects NOX2 (K_i = 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.

An orally bioavailable, non-toxic pyrazolopyridinedione based compound that acts as a potent and reversible inhibitor of NOX1- and NOX4-containing NADPH oxidase activity (K_i = 160 and 165 nM, respectively, Amplex Red assay) and devoid of antioxidant properties. At higher concentrations, affects NOX2 (K_i = 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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
NOX1- and NOX4-containing NADPH oxidase activity

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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.

その他情報

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.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable