| Bioactivity | 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[1]. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts[2]. | ||||||||||||
| Target | EC50: 45 nM (SUR2-KIR6). | ||||||||||||
| Invitro | P1075 (3 nM) induces monophasic inhibition curves by competition-binding experiments, in the presence of MgATP[1].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]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | P1075 (intravenous injection; 1μg/kg; once) treatment shows the reduction of infarct size in ischemia model[3]. Animal Model: | ||||||||||||
| Name | P-1075 | ||||||||||||
| CAS | 60559-98-0 | ||||||||||||
| Formula | C12H17N5 | ||||||||||||
| Molar Mass | 231.30 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Schwanstecher M, et al. Potassium channel openers require ATP to bind to and act through sulfonylurea receptors. EMBO J. 1998 Oct 1;17(19):5529-35. [2]. Oldenburg O, et al. P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts. J Mol Cell Cardiol. 2003 Sep;35(9):1035-42. [3]. Gross ER, et al. GSK3beta inhibition and K(ATP) channel opening mediate acute opioid-induced cardioprotection at reperfusion. Basic Res Cardiol. 2007 Jul;102(4):341-9. |