InChI
1S/C20H15BrN2O3/c21-18-6-2-1-5-17(18)20(25)14-7-9-16(10-8-14)26-13-19(24)23-15-4-3-11-22-12-15/h1-12H,13H2,(H,23,24)
InChI key
QNWXOXKHLFTJBA-UHFFFAOYSA-N
SMILES string
O=C(NC1=CC=CN=C1)COC2=CC=C(C(C3=C(Br)C=CC=C3)=O)C=C2
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
LUF7346 has the ability to enhance the potassium current (IKr) in a heterologous system. It is found to be highly effective than other human ether-a-go-go-related gene (hERG) activators, such as Rottlerin and NS1643.
LUF7346 is a Kv11.1 (hERG) allosteric modulator that prevents proarrhythmic effects caused by hERG blockers in rat ventricular myocyte cultures.
LUF7346 is a Kv11.1 (hERG) allosteric modulator that prevents proarrhythmic effects caused by hERG blockers in rat ventricular myocyte cultures. LUF7346 reduces Kv11.1 (ERG) affinity toward known Kv11.1 channel blockers dofetilide (Ki for hERG = 4.8 nM without and 12 nM with 10 μM LUF7346) and astemizole (Ki for for hERG = 1.3 nM without and 5.3 nM with 10 μM LUF7346) and effectively suppresses astemizole-induced arrhythmogenic events in a dose-dependent manner among Long-QT syndrome/LQTS (LQT1, JLNS, LQT2) and control isogenic human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). LUF7346 is shown to slow IKr deactivation and positively shifts IKr inactivation among LQTS and control isogenic hiPSC-CMs without affecting KCNQ1/KCNE1-dependent IKs or L-type calcium current ICaL.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Zhiyi Yu et al.
European journal of medicinal chemistry, 106, 50-59 (2015-11-01)
We synthesized and evaluated a series of compounds for their allosteric modulation at the Kv11.1 (hERG) channel. Most compounds were negative allosteric modulators of [(3)H]dofetilide binding to the channel, in particular 7f, 7h-j and 7p. Compounds 7f and 7p were
A new hERG allosteric modulator rescues genetic and drug-induced long-QT syndrome phenotypes in cardiomyocytes from isogenic pairs of patient induced pluripotent stem cells
Sala L, et al.
EMBO Molecular Medicine, 8(9), 1065-1081 (2016)
Luca Sala et al.
EMBO molecular medicine, 8(9), 1065-1081 (2016-07-30)
Long-QT syndrome (LQTS) is an arrhythmogenic disorder characterised by prolongation of the QT interval in the electrocardiogram, which can lead to sudden cardiac death. Pharmacological treatments are far from optimal for congenital forms of LQTS, while the acquired form, often
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