ML365 | Potent and selective K2P3.1 blocker
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $70.00 | ||
| 25 mg | $225.00 |
ML365 (947914-18-3) 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
References/Citations:
- 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
- Wu et al. (2022), ML365 inhibits TWIK2 channel to block ATP-induced NLRP3 inflammasome; Acta Pharmacol. Sin. 43 992
- Kim and Kang (2022), Blockade of TASK-1 Channel Improves the Efficacy of Levetiracetam in Chronically Epileptic Rats; Biomedicines 10 787
- Liu et al. (2022), ML365 inhibits liposaccharide-induced inflammatory responses via NF-kB signaling pathway; Immunobiology 227 152208
C22H20N2O3
>98% by HPLC
NMR: (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
ML365 (947914-18-3) 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
References/Citations:
- 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
- Wu et al. (2022), ML365 inhibits TWIK2 channel to block ATP-induced NLRP3 inflammasome; Acta Pharmacol. Sin. 43 992
- Kim and Kang (2022), Blockade of TASK-1 Channel Improves the Efficacy of Levetiracetam in Chronically Epileptic Rats; Biomedicines 10 787
- Liu et al. (2022), ML365 inhibits liposaccharide-induced inflammatory responses via NF-kB signaling pathway; Immunobiology 227 152208
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