Dofetilide

Catalog No.S1658 Batch:S165804

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Technical Data

Formula

C19H27N3O5S2
Molecular Weight 441.56 CAS No. 115256-11-6
Solubility (25°C)* In vitro DMSO 88 mg/mL (199.29 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
1.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 88 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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]

Protocol (from reference)

Selleck's Dofetilide has been cited by 6 publications

Identification of amitriptyline HCl, flavin adenine dinucleotide, azacitidine and calcitriol as repurposing drugs for influenza A H5N1 virus-induced lung injury. [ PLoS Pathog, 2020, 16;16(3):e1008341] PubMed: 32176725
Human ileal organoid model recapitulates clinical incidence of diarrhea associated with small molecule drugs [ Toxicol In Vitro, 2020, 104928] PubMed: 32622998
Clinical Trial in a Dish: Personalized Stem Cell-Derived Cardiomyocyte Assay Compared With Clinical Trial Results for Two QT-Prolonging Drugs. [ Clin Transl Sci, 2019, 12(6):687-697] PubMed: 31328865
Development and validation of a UPLC-MS/MS analytical method for dofetilide in mouse plasma and urine, and its application to pharmacokinetic study. [ J Pharm Biomed Anal, 2019, 172:183-188] PubMed: 31055183
Increased Late Sodium Current Contributes to the Electrophysiological Effects of Chronic, but Not Acute, Dofetilide Administration. [ Circ Arrhythm Electrophysiol, 2016, 9(4):e003655] PubMed: 27071826
Structural and functional screening in human induced-pluripotent stem cell-derived cardiomyocytes accurately identifies cardiotoxicity of multiple drug types. [Doherty KR, et al. Toxicol Appl Pharmacol, 2015, 285(1):51-60] PubMed: 25841593

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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