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A2793 is an efficient TWIK-related acid-sensitive K+ channel (TASK)-1 inhibitor, with an IC50 of 6.8 μM[1].

A2793 (100 µM) inhibits the unstimulated channel by 43.0±8.9% (n=5) while after ionomycin activation the reduction of the TRESK current is 85.5±2.9% (n=5)[1].A2793 may be considered as a tool to discriminate between the resting and activated channels in heterologous expression systems, and to block TRESK activated by calcineurin in the native cells which do not express TASK-1[1].

[1]. MiklÓs Lengyel, et al. Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K 2P 18.1) Background Potassium Channel. Mol Pharmacol. 2019 Jun;95(6):652-660.

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