For research use only. Not for therapeutic Use.
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].
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].
P1075 (intravenous injection; 1μg/kg; once) treatment shows the reduction of infarct size in ischemia model[3].
| Catalog Number | I008532 |
| CAS Number | 60559-98-0 |
| Synonyms | 1-cyano-2-(2-methylbutan-2-yl)-3-pyridin-3-ylguanidine |
| Molecular Formula | C12H17N5 |
| Purity | ≥95% |
| InChI | InChI=1S/C12H17N5/c1-4-12(2,3)17-11(15-9-13)16-10-6-5-7-14-8-10/h5-8H,4H2,1-3H3,(H2,15,16,17) |
| InChIKey | HKZNADVVGXKQDL-UHFFFAOYSA-N |
| SMILES | CCC(C)(C)N=C(NC#N)NC1=CN=CC=C1 |
| 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. |
