bl-1249

Description: BL-1249 is a novel, potent and selective K2P2.1 (TREK-1) and K2P10.1 (TREK-2) potassium channel activator. BL-1249 potently activates K2P2.1(TREK-1) and K2P10.1(TREK-2) with EC50 values of 5.5 uM and 8.0 uM, respectively. Extracellular application of BL-1249 activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 uM) than vascular tissue (EC50 of 21.0 uM).

References: Pope L, Arrigoni C, Lou H, Bryant C, Gallardo-Godoy A, Renslo AR, Minor DL Jr. Protein and Chemical Determinants of BL-1249 Action and Selectivity for K(2P) Channels.ACS Chem Neurosci. 2018 Dec 19; 9(12):3153-3165. Epub ahead of print PubMed PMID: 30089357; PubMed Central PMCID: PMC6302903; Iwaki Y, et al. Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249. Bioorg Med Chem Lett. 2019 Jul 1; 29(13):1601-1604.