产品
编 号:F403296
分子式:C12H17N5
分子量:231.3
产品类型
结构图
CAS No: 60559-98-0
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产品详情
生物活性:
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
体内研究:
P1075 (intravenous injection; 1μg/kg; once) treatment shows the reduction of infarct size in ischemia model.Animal Model:Male Sprague-Dawley rats subjected to 30 minutes of ischemia and 2 hours of reperfusion
Dosage:1μg/kg
Administration:Intravenous injection; 1μg/kg; once
Result:Reduced infarct size (41.8%) compared to the vehicle.
体外研究:
P1075 (3 nM) induces monophasic inhibition curves by competition-binding experiments, in the presence of MgATP.P1075 (100 μM; 10 min) leads to rabbit cardiomyocytes to produce ROS in a KATP-dependent fashion.P1075 (150 nM) reduces infarct size in isolated rabbit hearts compared to control animals (10.6% of the area at risk vs. 31.5%, P P-1075 相关抗体:Cell Viability AssayCell Line:COS-7 cells
Concentration:3-15 nM
Incubation Time:
Result:Showed IC50 value of 15 nM and Hill coefficient of 1.0.
Cell Viability AssayCell Line:Adult rabbit cardiomyocytes
Concentration:100 μM
Incubation Time:10 min
Result:Led to a 44% increase in ROS generation (P<0.001 vs. untreated cells).