LUF7244

Based on 20 reference(s) in Google Scholar 80 100 20

Axon 3032

CAS [1821638-43-0]

MF C20H15ClN2O3
MW 366.80

Purity: 98%
Soluble in DMSO

LUF7244

Description

LUF7244 is a potent negative allosteric modulator of Kv 11.1 (hERG) channels with an IC50 value of 3.9 μM. Moreover, LUF7244 was found to be a negative allosteric modulator of dofetilide (Axon 2103) binding to the Kv11.1 channel with the strongest effect at 10 μmol/L.

Z Yu et al. Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel. Eur J Med Chem. 2015 Dec 1;106:50-9.

Z Yu et al. Allosteric Modulation of Kv11.1 (hERG) Channels Protects Against Drug-Induced Ventricular Arrhythmias. Circ Arrhythm Electrophysiol. 2016;9(4).

M Qile et al. LUF7244, an Allosteric Modulator/Activator of K v 11.1 Channels, Counteracts Dofetilide-Induced Torsades De Pointes Arrhythmia in the Chronic Atrioventricular Block Dog Model. Br J Pharmacol. 2019;176(19):3871-3885.

Cardiovascular Kv11.1 KCNH2

Potent negative allosteric modulator (NAM) of the Kv11.1 (hERG) channel

Chemical name

2-(4-(3-Chlorobenzoyl)phenoxy)-N-(pyridin-3-yl)acetamide

Parent CAS No.

[1821638-43-0]

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Axon ID	Name	Description	From price
2103	Dofetilide	Kv11.1 (hERG) channel blocker		€85.00
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LUF7244

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LUF7244

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