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LUF7244
Axon 3032
CAS:
1821638-43-0
Purity:
98%
- Soluble in DMSO
- MF: C20H15ClN2O3
- MW: 366.8
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.
More Information
| Parent CAS No. | 1821638-43-0 |
|---|---|
| Chemical Name | 2-(4-(3-Chlorobenzoyl)phenoxy)-N-(pyridin-3-yl)acetamide |
| SMILES | C1C=CC(NC(=O)COC2C=CC(C(=O)C3C=CC=C(Cl)C=3)=CC=2)=CN=1 |
| MFCD | N.A. |
| 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) |
| InChiKey | KKKJYDOHVKIIQP-UHFFFAOYSA-N |
| CID | 127042386 |
| Short Description | Kv11.1 channel NAM |
References
- 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.
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