Home Transmembrane Transporters Potassium Channel inhibitor Dofetilide For research use only.

Dofetilide

Synonyms: UK-68798

Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.

Dofetilide Chemical Structure

Dofetilide Chemical Structure

CAS No. 115256-11-6

Purity & Quality Control

Dofetilide Related Products

Signaling Pathway

Potassium Channel Signaling Pathways

Potassium Channel Signaling Pathway

Biological Activity

Description Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.
Targets
Potassium channel [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05906732 Recruiting
Long QT Syndrome
Thryv Therapeutics Inc.
 March 12 2023 Phase 1|Phase 2
NCT01097330 Terminated
Defibrillators Implantable|Tachycardia Ventricular
Population Health Research Institute|Abbott Medical Devices|Hamilton Health Sciences Corporation
 August 2010 Phase 3

Chemical Information & Solubility

Molecular Weight 441.56 Formula

C19H27N3O5S2
CAS No. 115256-11-6 SDF Download Dofetilide SDF
Smiles CN(CCC1=CC=C(C=C1)NS(=O)(=O)C)CCOC2=CC=C(C=C2)NS(=O)(=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (199.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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