P1075

P1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-K_ir6) with an EC₅₀ value of 45 nM for SUR2B-K_ir6 channel activation.¹ It is highly selective for SUR2 over SUR1 isoforms (IC₅₀s = 9-46 nM and 1.02 mM, respectively, in a radioligand binding assay). P1075 increases outflow facility, a marker of reduced intraocular pressure, in human eye anterior segments ex vivo.² It also reduces infarct size in isolated rabbit hearts via activation of mitochondrial ATP-sensitive potassium channels (K_ATP; EC₅₀s = 60-90 nM).³

WARNING This product is not for human or veterinary use.

1. Schwanstecher, M., Sieverding, C., Dörschner, H., et al. Potassium channel openers require ATP to bind to and act through sulfonylurea receptors. EMBO J. 17(19), 5529-5535 (1998).

2. Chowdhury, U.R., Bahler, C.K., Hann, C.R., et al. ATP-sensitive potassium (KATP) channel activation decreases intraocular pressure in the anterior chamber of the eye. Invest. Ophthalmol. Vis. Sci. 52(9), 6435-6442 (2011).

3. Oldenburg, O., Yang, X.M., Krieg, T., et al. P1075 opens mitochondrial KATP channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts. J. Mol. Cell. Cardiol. 35(9), 1035-1042 (2003).