| Identification | Back Directory | [Name]
Acetamide, 2-[4-(3-chlorobenzoyl)phenoxy]-N-3-pyridinyl- | [CAS]
1821638-43-0 | [Synonyms]
LUF7244
Acetamide, 2-[4-(3-chlorobenzoyl)phenoxy]-N-3-pyridinyl- | [Molecular Formula]
C20H15ClN2O3 | [MOL File]
1821638-43-0.mol | [Molecular Weight]
366.8 |
| Chemical Properties | Back Directory | [Boiling point ]
629.5±55.0 °C(Predicted) | [density ]
1.337±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
12.13±0.70(Predicted) | [color ]
white to beige | [InChIKey]
KKKJYDOHVKIIQP-UHFFFAOYSA-N | [SMILES]
O=C(NC1=CC=CN=C1)COC2=CC=C(C=C2)C(C3=CC=CC(Cl)=C3)=O |
| Hazard Information | Back Directory | [Uses]
LUF7244 is a selective allosteric modulator of Kv11.1 channels. LUF7244 inhibits early afterdepolarizations. LUF7244 can be used for anti-arrhythmia research[1]. | [Biological Activity]
LUF7244 is a potent and selective voltage-gated potassium 11.1 (Kv11.1) channels negative allosteric modulator/activator th at inhibits early afterdepolarizations in vitro. It decreases the affinity of Kv11.1 for cisaprideastemizoledofetilide and sertindole. LUF7244 averts dofetilide‐induced torsades de pointes arrhythmias in dogs with chronic atrioventricular block. LUF7244 in combination with dofetilide rescues both congenital and acquired Kv11.1 trafficking defects and produces functional Kv11.1 current in trafficking defective G601S-Kv11.1 cells. | [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]. | [References]
[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. DOI:10.1111/bph.14798 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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