PeptideDB

LUF7244

CAS: 1821638-43-0 F: C20H15ClN2O3 W: 366.80

LUF7244 is a selective allosteric modulator of Kv11.1 channels. LUF7244 inhibits early afterdepolarizations. LUF7244 can
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Bioactivity LUF7244 is a selective allosteric modulator of Kv11.1 channels. LUF7244 inhibits early afterdepolarizations. LUF7244 can be used for anti-arrhythmia research[1].
Invitro LUF7244 (0-10 μM; HEK293 cells) binds Kv11.1 channels and increases IKv11.1 by inhibiting inactivation in a dose-dependent manner[1].LUF7244 (0-10 μM; cardiomyocytes) reduces action potential duration (APD) by approximately 50% and dofetilide-induced early afterdepolarization (EAD) in isolated ventricular CMCs from SR and CAVB dogs[1].LUF7244 (10 μM) had no effects on IKIR2.1, INav1.5, ICa-L, and IKs but doubled IKr[1].
In Vivo LUF7244 (2.5 mg/kg; i.v.; for 15 min) decreases repolarization parameters. LUF7244 has antiarrhythmic effects against dofetilide-induced TdP arrhythmias in CAVB dogs[1].
Name LUF7244
CAS 1821638-43-0
Formula C20H15ClN2O3
Molar Mass 366.80
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Qile M, et, al. LUF7244, an allosteric modulator/activator of Kv 11.1 channels, counteracts dofetilide-induced torsades de pointes arrhythmia in the chronic atrioventricular block dog model. Br J Pharmacol. 2019 Oct;176(19):3871-3885.