Potent Kv7.1 activator / ML277 is a potent (EC50 = 260 nM) activator of Kv7.1 with selectivity against Kv7.2, Kv7.4, and Kv11.1 (hERG).1 ML277 enhances cardiac delayed rectifier K+ currents (IKs) in human iPSC-derived cardiomyocytes from normal and long QT-interval syndrome afflicted patients suggesting potential therapeutic use in long QT-interval syndrome.2,3 It displayed cardioprotective effects against ischemia in cellular and whole-heart models.4
Biochemicals & reagents
1401242-74-7
(R)-N-(4-(4-Methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide
1) Mattman et al. (2012) Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent, and selective K(v)7.1(KCNQ1 potassium channel activator; Bioorg. Med. Chem. Lett. 22 5936 2) Yu et al. (2013) Dynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels; Proc. Nat. Acad. Sci. USA 110 8732 3) Ma et al. (2015) Characterization of a novel KCNQ1 mutation for type 1 long QT syndrome and assessment of the therapeutic potential of a novel IKs activator using patient-specific induced pluripotent stem cell-derived cardiomyocytes; Stem Cell Res. Ther. 6 39 4) Brennan et al. (2023) Slowly activating voltage-gated potassium current potentiation by ML277 is a novel cardioprotective intervention; PNAS Nexus 2 pgad156
-20°C
TARGET: Ion channel -- PATHWAY: Cation channel -- DISEASE AREA: Heart disease; Ischemia