GSK2795039

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GSK2795039  纯度: 99.71%

GSK2795039 是一种 NADPH 氧化酶 2 (NOX2) 抑制剂，在不同的无细胞试验中平均 pIC50 为 6。GSK2795039 抑制活性氧 (Reactive Oxygen Species) 产生和 NADPH 消耗，同时可减少细胞凋亡 (apoptosis)。

GSK2795039

GSK2795039 Chemical Structure

CAS No. : 1415925-18-6

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥3190 In-stock
5 mg ￥2900 In-stock
10 mg ￥4200 In-stock
25 mg ￥8400 In-stock
50 mg ￥13400 In-stock
100 mg ￥21500 In-stock
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500 mg   询价  

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生物活性

GSK2795039 is a NADPH oxidase 2 (NOX2) inhibitor with a mean pIC50 of 6 in different cell-free assays. GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption[1]. GSK2795039 reduces apoptosis[2].

体外研究
(In Vitro)

GSK2795039 (25 μM; 24 hours) reduces the combinatory effect of FeSO4 and LPS-increased levels of apoptosis and reduced the presence of caspase-3-positive PC12 cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[2]

Cell Line: PC12 cells
Concentration: 25 μM
Incubation Time: 24 hours
Result: Reduced apoptosis among PC12 cells.

体内研究
(In Vivo)

GSK2795039 (intraperitoneal injection; 100 mg/kg; 1 hour before) decreases activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL6 mice[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection; 100 mg/kg; 1 hour before
Result: Caused 50% reduction in the level of serum amylase activity.

分子量

450.56

Formula

C23H26N6O2S
CAS 号

1415925-18-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (221.95 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2195 mL 11.0973 mL 22.1946 mL
5 mM 0.4439 mL 2.2195 mL 4.4389 mL
10 mM 0.2219 mL 1.1097 mL 2.2195 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 20% DMSO, 20% Tween 80, 60% polyethylene glycol 200

    Solubility: 10 mg/mL (22.19 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 15% Cremophor EL    85% Saline

    Solubility: 6.67 mg/mL (14.80 mM); Suspended solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.55 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 4.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.55 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Hirano K, et al. Discovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibitor. Antioxid Redox Signal. 2015 Aug 10;23(5):358-74.

    [2]. Yauger YJ, 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.

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