For research use only. Not for therapeutic Use.
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.
KEYWORDS: LUF7244 | supplier | Kv11.1 channel NAM | LUF 7244 | LUF-7244 | CAS [1821638-43-0] | Potassium | Kv11.1 | NAM | Ion Channels | Ventricular arrhythmia | Afterdepolarization | Torsades de pointes arrhythmia
| Catalog Number | I047641 |
| CAS Number | 1821638-43-0 |
| Molecular Formula | C20H15ClN2O3 |
| Purity | ≥95% |
| IUPAC Name | 2-[4-(3-chlorobenzoyl)phenoxy]-N-pyridin-3-ylacetamide |
| InChI | InChI=1S/C20H15ClN2O3/c21-16-4-1-3-15(11-16)20(25)14-6-8-18(9-7-14)26-13-19(24)23-17-5-2-10-22-12-17/h1-12H,13H2,(H,23,24) |
| SMILES | C1=CC(=CC(=C1)Cl)C(=O)C2=CC=C(C=C2)OCC(=O)NC3=CN=CC=C3 |
| Reference | 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. |
