WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555142
Description: ML365 is a potent and selective K2P3.1 TASK-1 channel blocker. ML365 blocks TASK1 channels in both the thallium influx fluorescent assay (IC50 = 4 nM) and an automated electrophysiology assay (IC50 = 16 nM). Based on potency differences, it possesses more than 60-fold selectivity for inhibition of TASK1 over a closely-related, two-pore domain potassium channel, TASK3. ML365 displays little or no inhibition at 30 μM of more distantly related potassium channels, Kir2.1, potassium voltage-gated channel, KQT-like subfamily, member 2 (KCNQ2), and human ether-a go-go-related gene (hERG). Based on these criteria, ML365 is a best-in-class probe and is a useful pharmacological probe for in vitro studies of TASK1 function and in further studies aimed at developing therapeutic intervention.
MedKoo Cat#: 555142
Chemical Formula: C22H20N2O3
Exact Mass: 360.1474
Molecular Weight: 360.413
Elemental Analysis: C, 73.32; H, 5.59; N, 7.77; O, 13.32
Synonym: ML365; ML-365; ML 365;
IUPAC/Chemical Name: 2-Methoxy-N-[3-[(3-methylbenzoyl)amino]phenyl]benzamide
InChi Key: UTAJHKSGYJSZBR-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H20N2O3/c1-15-7-5-8-16(13-15)21(25)23-17-9-6-10-18(14-17)24-22(26)19-11-3-4-12-20(19)27-2/h3-14H,1-2H3,(H,23,25)(H,24,26)
SMILES Code: O=C(NC1=CC=CC(NC(C2=CC=CC(C)=C2)=O)=C1)C3=CC=CC=C3OC
1: Skarsfeldt MA, Jepps TA, Bomholtz SH, Abildgaard L, Sørensen US, Gregers E,
Svendsen JH, Diness JG, Grunnet M, Schmitt N, Olesen SP, Bentzen BH. pH-dependent
inhibition of K₂P3.1 prolongs atrial refractoriness in whole hearts. Pflugers
Arch. 2016 Apr;468(4):643-54. doi: 10.1007/s00424-015-1779-0. Epub 2016 Jan 5.
PubMed PMID: 26729267.
2: Zou B, Flaherty DP, Simpson DS, Maki BE, Miller MR, Shi J, Wu M, McManus OB,
Golden JE, Aubé J, Li M. ML365: Development of Bis-Amides as Selective Inhibitors
of the KCNK3/TASK1 Two Pore Potassium Channel. 2013 Apr 15 [updated 2013 Nov 14].
Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD):
National Center for Biotechnology Information (US); 2010-. Available from
PubMed PMID: 24479195.