GSK2795039

用途生物活性靶点体外研究体内研究 GSK2795039 试剂级价格

GSK2795039

CAS号:1415925-18-6
英文名:GSK2795039
中文名:GSK2795039
CBNumber:CB13152080
分子式:C23H26N6O2S
分子量:450.56
MOL File:1415925-18-6.mol

GSK2795039化学性质

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(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)
形态 :A solid
酸度系数(pKa) :6.99±0.30(Predicted)
颜色 :White to yellow
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性质、用途与生产工艺

用途
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。
生物活性 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
Target Value
ROS
()
NADPH
()
NOX2 (HRP/Amplex Red)
(Cell-based assay) 6.57(pIC50)

体外研究

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.

体内研究

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.