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A2764 is an inhibitor of the two-pore domain potassium channel K2P18.1/TRESK (IC50 = 11.8 µM in ionomycin-stimulated Xenopus oocytes expressing the mouse receptor).1 It is selective for K2P18.1/TRESK over K2P2.1/TREK1, K2P10.1/TREK2, K2P4.1/TRAAK, K2P3.1/TASK1, K2P3.2/TASK2, K2P3.3/TASK3, K2P16.1/TALK1, and K2P13.1/THIK1 at 100 µM. A2764 (100 µM) inhibits basal potassium currents in isolated mouse dorsal root ganglion neurons.
WARNING This product is not for human or veterinary use.
1. Chemically modified derivatives of the activator compound cloxyquin exert inhibitory effect on TRESK (K2P18.1) background potassium channel. Mol. Pharmacol. 95(6), 652-660 (2019).