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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.
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.
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