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Dofetilide

Catalog No. T6476 CAS 115256-11-6

Synonyms: UK 68789, UK-68798, Tikosyn

Dofetilide (UK 68789) is a sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter.

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Dofetilide, CAS 115256-11-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 50.00
10 mg	In stock	$ 63.00
25 mg	In stock	$ 119.00
50 mg	In stock	$ 187.00
100 mg	In stock	$ 263.00
200 mg	In stock	$ 506.00
500 mg	In stock	$ 823.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.06%

Purity: 98.69%

Purity: 96.97%

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Storage & Solubility Information

Description	Dofetilide (UK 68789) is a sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter.
In vitro	Dofetilide blocks HERG currents in excised macro patches of Xenopus oocytes. [1] Dofetilide (1 μM) reduces 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. [2] Dofetilide increases apico-basal disparity of repolarization, due to a more marked increase of ERPs in the apex than in the base in the intact canine heart. [3]
In vivo	Dofetilide (100 mg/kg, i.v.) does not suppress automaticity arrhythmias induced by two-stage coronary ligation and epinephrine or the coronary ligation and reperfusion arrhythmias, but suppresses the reentry arrhythmia induced by PES in dogs with old myocardial infarction (MI). Dofetilide also shows antiarrhythmic effect in some dogs with digitalis arrhythmia. Dofetilide increases QT interval and shows negative chronotropic effect like that of other class III drugs, but is different in antiarrhythmic profiles from those of other class III agents such as D-sotalol, E-4031, and MS-551 in that it does not prevent the occurrence of ventricular fibrillation (VF) immediately after coronary reperfusion and has some antiarrhythmic effects on digitalis arrhythmia. [4] Dofetilide causes increased resorptions and the same stage-dependent malformations in Sprague-Dawley rats. [5]

Synonyms	UK 68789, UK-68798, Tikosyn
Molecular Weight	441.56
Formula	C19H27N3O5S2
CAS No.	115256-11-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 44.2 mg/mL (100 mM)

References and Literature

1. Kiehn J, et al. Circulation, 1996, 94(10), 2572-2579. 2. Kiehn J, et al. J Cardiovasc Pharmacol, 1994, 24(4), 566-572. 3. Bauer A, et al. J Cardiovasc Pharmacol, 2002, 39(3), 460-467. 4. Chen J, et al. J Cardiovasc Pharmacol, 1996, 28(4), 576-584. 5. Webster WS, et al. Teratology, 1996, 53(3), 168-175.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library EMA Approved Drug Library Anti-Cancer Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Target-Focused Phenotypic Screening Library ReFRAME Related Library Ion Channel Inhibitor Library FDA-Approved Drug Library

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Keywords

Dofetilide 115256-11-6 Membrane transporter/Ion channel Potassium Channel cardiovascular UK68798 UK68789 potent specific class antiarrhythmic UK 68789 UK-68798 orally UK-68789 Inhibitor Tikosyn inhibit KcsA UK 68798 III agent inhibitor

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