1415925-18-6
中文名稱
1415925-18-6
英文名稱
GSK2795039
CAS
1415925-18-6
分子式
C23H26N6O2S
分子量
450.56
MOL 文件
1415925-18-6.mol
更新日期
2024/12/23 17:39:04
1415925-18-6 結(jié)構(gòu)式
基本信息
中文別名
化合物GSK2795039NOX2抑制劑(GSK2795039)
英文別名
GSK2795039GSK-2795039 (GSK 2795039
N-(1-isopropyl-3-(1-methylindolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-methyl-1H-pyrazole-3-sulfonamide
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-
所屬類別
生物化工：抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)691.5±65.0 °C(Predicted)
密度1.39±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
儲(chǔ)存條件Sealed in dry,2-8°C
溶解度DMF:30.0(Max Conc. mg/mL);66.58(Max Conc. mM)
DMSO:66.27(Max Conc. mg/mL);147.07(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.44(Max Conc. mM)
Ethanol:20.0(Max Conc. mg/mL);44.39(Max Conc. mM)
DMSO:66.27(Max Conc. mg/mL);147.07(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.44(Max Conc. mM)
Ethanol:20.0(Max Conc. mg/mL);44.39(Max Conc. mM)
酸度系數(shù)(pKa)6.99±0.30(Predicted)
形態(tài)固體
顏色White to yellow
InChIKeyFMWVTCZKCXPKFW-UHFFFAOYSA-N
SMILESN1(C)C=CC(S(NC2C=CN=C3N(C(C)C)C=C(C4=CC5=C(C=C4)CCN5C)C3=2)(=O)=O)=N1
常見(jiàn)問(wèn)題列表
用途
GSK2795039是NADPHoxidase2(NOX2)的抑制劑，可抑制活性氧reactiveoxygenspecies(ROS)的產(chǎn)生，NADPH的消耗并減少細(xì)胞凋亡。
生物活性
GSK2795039 是 NADPH oxidase 2 (NOX2) 的抑制劑，對(duì)于NOX2介導(dǎo)的HRP/Amplex Red的激活的pIC50值為6.57。GSK2795039 可抑制活性氧reactive oxygen species (ROS)的產(chǎn)生，NADPH的消耗并減少細(xì)胞凋亡。靶點(diǎn)
| Target | Value |
|
ROS
() | |
|
NADPH
() | |
|
NOX2 (HRP/Amplex Red)
(Cell-based assay) | 6.57(pIC50) |
體外研究
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. |
體內(nèi)研究
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. |