BL-1249 is a selective opener of the TREK-1 (K2P2.1) and TREK-2 (K2P10.1) potassium channels, demonstrating potent activation with EC50 values of 5.5 μM and 8.0 μM, respectively. This compound effectively activates all members of the TREK subfamily while exhibiting no activity towards other K2P subfamilies. Notably, BL-1249 shows enhanced selectivity for bladder tissue, with an EC50 of 1.26 μM, compared to a higher EC50 of 21.0 μM in vascular tissue. The compound is valuable in research related to pain management and bladder function regulation.
BL-1249 is a selective opener of the TREK-1 (K2P2.1) and TREK-2 (K2P10.1) potassium channels, demonstrating potent activation with EC50 values of 5.5 μM and 8.0 μM, respectively. This compound effectively activates all members of the TREK subfamily while exhibiting no activity towards other K2P subfamilies. Notably, BL-1249 shows enhanced selectivity for bladder tissue, with an EC50 of 1.26 μM, compared to a higher EC50 of 21.0 μM in vascular tissue. The compound is valuable in research related to pain management and bladder function regulation.
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