GSK2795039
| 中文名称 | GSK2795039 |
|---|---|
| 中文同义词 | NOX2抑制剂(GSK2795039);化合物GSK2795039;N-(1-异丙基-3-(1-甲基吲哚啉-6-基)-1H-吡咯[2,3-B]吡啶-4-基)-1-甲基-1H-吡唑-3-磺酰胺;化合物GSK2795039,10 MM DMSO 溶液;GSK2795039 ,S8974;GSK2795039 抑制剂;GSK2795039试剂;GSK2795039 抑制剂 |
| 英文名称 | GSK2795039 |
| 英文同义词 | GSK2795039;N-(1-isopropyl-3-(1-methylindolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-methyl-1H-pyrazole-3-sulfonamide;GSK-2795039 (GSK 2795039;1H-Pyrazole-3-sulfonamide, N-[3-(2,3-dihydro-1-methyl-1H-indol-6-yl)-1-(1-methylethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-methyl-;Inhibitor,Reactive Oxygen Species,NADPH Oxidase,NOX,inhibit,Apoptosis,GSK-2795039,GSK2795039,GSK 2795039;GSK2795039, 10 mM in DMSO;GSK2795039 ，S8974 |
| CAS号 | 1415925-18-6 |
| 分子式 | C23H26N6O2S |
| 分子量 | 450.56 |
| EINECS号 | |
| 相关类别 | 抑制剂;细胞生物学试剂 |
| Mol文件 | 1415925-18-6.mol |
| 结构式 |  |
GSK2795039 性质
| 沸点 | 691.5±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.39±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMF:30.0(最大浓度 mg/mL);66.58(最大浓度 mM) DMSO:66.27(最大浓度 mg/mL);147.07(最大浓度 mM) DMSO:PBS ( pH 7.2) (1:4):0.2(最大浓度 mg/mL);0.44(最大浓度 mM) 乙醇:20.0(最大浓度 mg/mL);44.39(最大浓度 mM) |
| 形态 | 固体 |
| 酸度系数(pKa) | 6.99±0.30(Predicted) |
| 颜色 | 白色至黄色 |
| InChIKey | FMWVTCZKCXPKFW-UHFFFAOYSA-N |
| SMILES | N1(C)C=CC(S(NC2C=CN=C3N(C(C)C)C=C(C4=CC5=C(C=C4)CCN5C)C3=2)(=O)=O)=N1 |
GSK2795039是NADPHoxidase2(NOX2)的抑制剂，可抑制活性氧reactiveoxygenspecies(ROS)的产生，NADPH的消耗并减少细胞凋亡。
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。| Target | Value |
|
ROS
() | |
|
NADPH
() | |
|
NOX2 (HRP/Amplex Red)
(Cell-based assay) | 6.57(pIC50) |
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.
Apoptosis Analysis
| Cell Line: | PC12 cells |
| Concentration: | 25 μM |
| Incubation Time: | 24 hours |
| Result: | Reduced apoptosis among PC12 cells. |
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.
| Animal Model: | C57BL6 mice |
| Dosage: | 100 mg/kg |
| Administration: | Intraperitoneal injection; 100 mg/kg; 1 hour before |
| Result: | Caused 50% reduction in the level of serum amylase activity. |
安全信息
| WGK Germany | WGK 3 |
|---|---|
| 存储类别 | 11 - 可燃固体 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/07/06 | S8974 | 1415925-18-6 GSK2795039 | 1415925-18-6 | 5mg | 2370元 |
| 2026/07/06 | S8974 | GSK2795039 | 1415925-18-6 | 10mM (1mL in DMSO) | 2970元 |