货号	规格	价格	上海	北京	珠海	重庆	武汉
S83211-1mg促销	≥97%	￥160.00 ￥140.00 S83211-1mg ￥140.00 2-3天	0 货期：2-3天	-	-	-	-
S83211-5mg买3赠1	97.60%	￥280.00 S83211-5mg ￥280.00 现货（买3赠1）	6 6	-	-	-	-
S83211-10mg	97.60%	￥420.00 S83211-10mg ￥420.00 现货	3 3	-	-	-	-
S83211-50mg	97.60%	￥750.00 S83211-50mg ￥750.00 现货	1 1	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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