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Dofetilide Potassium Channel inhibitor

Cat.No.S1658

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

Batch: Purity: 100.00%
100.00

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (199.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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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Chemical Information, Storage & Stability

Molecular Weight 441.56 Formula

C19H27N3O5S2

Storage (From the date of receipt)
CAS No. 115256-11-6 Download SDF Storage of Stock Solutions

Synonyms UK-68798 SMILES CN(CCC1=CC=C(C=C1)NS(=O)(=O)C)CCOC2=CC=C(C=C2)NS(=O)(=O)C

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Mechanism of Action

Targets/IC50/Ki
Potassium channel
In vitro
Dofetilide blocks HERG currents in excised macro patches of Xenopus oocytes. This compound (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. It 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.
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). This compound also shows antiarrhythmic effect in some dogs with digitalis arrhythmia. It 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. This chemical causes increased resorptions and the same stage-dependent malformations in Sprague-Dawley rats.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/8891885/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8761884/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-28)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06096337 ACTIVE_NOT_RECRUITING
Persistent Atrial Fibrillation
Boston Scientific Corporation
2023-12-28
NCT05906732 TERMINATED
Long QT Syndrome
Thryv Therapeutics, Inc.
2023-03-12 PHASE1; PHASE2
NCT05906732 Recruiting
Long QT Syndrome
Thryv Therapeutics Inc.
2023-03-12 Phase 1|Phase 2
NCT03070470 COMPLETED
Drug-induced QT Prolongation; Pharmacokinetics; Pharmacodynamics
Food and Drug Administration (FDA)
2017-03-14 PHASE1
NCT02365532 COMPLETED
Long QT Syndrome
Gilead Sciences
2015-02 PHASE1
NCT02308748 COMPLETED
Drug-induced QT Prolongation; Pharmacokinetics; Pharmacodynamics
Food and Drug Administration (FDA)
2014-05 PHASE1

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