GSK2795039
目录号 : GC32681
A NOX2 inhibitor
Cas No.:1415925-18-6
Sample solution is provided at 25 µL, 10mM.
GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2; IC50 = 0.269 ?M).1 It is selective for NOX2 over NOX1, -3, -4, and -5 (IC50s = >1,000 ?M for all), as well as xanthine oxidase and PKCβ (IC50s = 28.8 and 10 ?M, respectively). GSK2795039 inhibits NOX2-mediated production of reactive oxygen species (ROS) and NADPH depletion in cell-free assays (IC50s = 0.537 and 0.251 ?M, respectively). In vivo, GSK2795039 (100 mg/kg) reduces serum levels of amylase, a marker for pancreatic cell necrosis, in a gp91phox knockout mouse model of acute pancreatitis. GSK2795039 also inhibits brain NOX2 activity, decreases neurite shortening and apoptosis, and attenuates neurological deficits in a mouse model of weight drop-induced traumatic brain injury (TBI).2
1.Hirano, K., Chen, W.S., Chueng, A.L.W., et al.Discovery of GSK2795039, a novel small molecule NADPH oxidase 2 inhibitorAntioxid. Redox Signal.23(5)(2015) 2.Wang, M., and Luo, L.An effective NADPH oxidase 2 inhibitor provides neuroprotection and improves functional outcomes in animal model of traumatic brain injuryNeurochem. Res.45(5)1097-1106(2020)
| Cas No. | 1415925-18-6 | SDF | |
| Canonical SMILES | CC(C)N1C=C(C2=CC=C(CCN3C)C3=C2)C4=C1N=CC=C4NS(C5=NN(C)C=C5)(=O)=O | ||
| 分子式 | C23H26N6O2S | 分子量 | 450.56 |
| 溶解度 | DMSO : ≥ 32 mg/mL (71.02 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet