ML365
Potent and selective K2P3.1 blocker / ML365 is a potent (IC50 = 16 nM) and selective (62-fold selective over TASK-3) blocker of the two-pore domain potassium channel K2P3.1 (TASK-1) .1 It also less potently (IC50 = 4.07 µM) blocks the K2P6.1 (TWIK-2) channel resulting in blocking the ATP-induced NLRP3 inflammasome.2 ML365 improved the efficacy of Levetiracetam in chronically epileptic rats.3 It suppressed the release of TNF-α, IL-6, and IL-1ß in an LPS-induced inflammatory model via regulation of NF-kB signaling.4
Biochemicals & reagents
947914-18-3
1) Flaherty et al. (2014), Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold; Bioorg. Med. Chem. Lett. 24 3968 2) Wu et al. (2022), ML365 inhibits TWIK2 channel to block ATP-induced NLRP3 inflammasome; Acta Pharmacol. Sin. 43 992 3) Kim and Kang (2022), Blockade of TASK-1 Channel Improves the Efficacy of Levetiracetam in Chronically Epileptic Rats; Biomedicines 10 787 4) Liu et al. (2022), ML365 inhibits liposaccharide-induced inflammatory responses via NF-kB signaling pathway; Immunobiology 227 152208
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TARGET: Ion channel; Inflammasome -- PATHWAY: Cation channel; NFkappaB; TNF -- DISEASE AREA: Inflammation