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• 产品描述： GSK2795039 是 NADPH oxidase 2 (NOX2) 的抑制剂，对于NOX2介导的HRP/Amplex Red的激活的pIC50值为6.57。GSK2795039 可抑制活性氧reactive oxygen species (ROS)的产生，NADPH的消耗并减少细胞凋亡

• 靶点： ROS; NADPH; NOX2(HRP/Amplex Red)(Cell-based assay):6.57(pIC50);Apoptosis; ReactiveOxygenSpecies; ROS; NADPH

• 体外研究：
  GSK2795039 inhibits both the formation of ROS and the utilization of the enzyme substrates, NADPH and oxygen, in a variety of semirecombinant cell-free and cell-based NOX2 assays. GSK2795039 inhibits NOX2 in an NADPH competitive manner and is selective over other NOX isoforms, xanthine oxidase, and endothelial nitric oxide synthase enzymes

• 体内研究：
  Following systemic administration in mice, GSK2795039 abolishes the production of ROS by activated NOX2 enzyme in a paw inflammation model. GSK2795039 shows activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein

• 细胞实验： Cell lines: NOX isoform-specific cells, PBMCs, PMNs, HL60 cells Concentrations: 3.16 nM, 10 nM, 31.6 nM, 100 nM, 316 nM, 1μM, 3.16 μM, 10 μM, 31.6 μM, 100μM Incubation Time: 10 min, 20 min, 30 min, 40 min, 50 min, 60 min Method: For Amplex Red/HRP assay, cells are preincubated with the GSK2795039 for 10 min at room temperature in PerkinElmer black 96-well microplates at 50,000 cells per well, after which the reaction mixture is added to a final concentration of 25 μM of Amplex Red and 0.05 U/ml of HRP in HBSS. NOX enzymes are activated via 100 nM PMA (NOX1, NOX2), 1 μg/ml tetracycline for 24-h activation of inducible genes (NOX3, NOX4), and 1 μM Ca2+ ionophore ionomycin (NOX5).

• 动物实验： Animal Models: Male Sprague-Dawley (SD) rats, C57BL6/J mice, gp91phox knockout mice Dosages: 2–100 mg/kg Administration: IP

• 参考文献：
  1. Kazufumi Hirano, et al. Discovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibitor. Antioxid Redox Signal. 2015 Aug 10;23(5):358-74. 2. Young J Yauger, et al. Iron accentuated reactive oxygen species release by NADPH oxidase in activated microglia contributes to oxidative stress in vitro. J Neuroinflammation. 2019 Feb 18;16(1):41.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.219 ml	11.097 ml	22.195 ml
  5 mM	0.444 ml	2.219 ml	4.439 ml
  10 mM	0.222 ml	1.11 ml	2.219 ml
  50 mM	0.044 ml	0.222 ml	0.444 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *