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Dofetilide

In stock
Catalog No.
A8417
Potassium channel inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$60.00
In stock
10mg
$60.00
In stock

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Background

Dofetilide is a potassium channel blocker.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt441.56
Cas No.115256-11-6
FormulaC19H27N3O5S2
Solubility≥21.15mg/mL in DMSO
Chemical NameN-[4-[2-[2-[4-(methanesulfonamido)phenoxy]ethyl-methylamino]ethyl]phenyl]methanesulfonamide
SDFDownload SDF
Canonical SMILESCN(CCC1=CC=C(C=C1)NS(=O)(=O)C)CCOC2=CC=C(C=C2)NS(=O)(=O)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1,2]:

Cell lines

HEK293 cells, guinea pig cardiomyocytes

Preparation method

The solubility of this compound in DMSO is >21.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 μM

Applications

In a human cell line and human embryonic kidney 293 transfected with HERG, dofetilide induced channel block with the EC50 of 12 ± 2 nM. Induction of block depended on depolarization beyond the threshold for channel opening. Dofetilide acted as a slow-onset/slow-offset open channel blocker of this current at nanomolar concentrations. Dofetilide (1 μM) reduced the amplitude of IKr to 61% of control currents in guinea pig cardiomyocytes, as measured by 200-ms test pulses and analysis of the deactivating tail currents of IKr.

Animal experiment [3]:

Animal models

Dogs with old myocardial infarction (MI)

Dosage form

Intravenous injection, 100 mg/kg

Application

Dofetilide (100 mg/kg, i.v.) suppressed the reentry arrhythmia induced by PES in dogs with old myocardial infarction (MI). Dofetilide showed antiarrhythmic effect in some dogs with digitalis arrhythmia. Dofetilide increased QT interval and showed negative chronotropic effect.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Snyders D J, Chaudhary A. High affinity open channel block by dofetilide of HERG expressed in a human cell line[J]. Molecular Pharmacology, 1996, 49(6): 949-955.

[2]. Kiehn J, Villena P, Beyer T, et al. Differential effects of the new class III agent dofetilide on potassium currents in guinea pig cardiomyocytes[J]. Journal of cardiovascular pharmacology, 1994, 24(4): 566-572.

[3]. Chen J, Xue Y, Eto K, et al. Effects of dofetilide, a class III antiarrhythmic drug, on various ventricular arrhythmias in dogs[J]. Journal of cardiovascular pharmacology, 1996, 28(4): 576-584.

Quality Control

Chemical structure

Dofetilide

Related Biological Data

Dofetilide

Related Biological Data

Dofetilide