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[2].IC50 & Target:EC50: 45 nM (SUR2-KIR6).In Vitro: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[2].
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 < 0.05)[2].In Vivo:P1075 (intravenous injection; 1μg/kg; once) treatment shows the reduction of infarct size in ischemia model.