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    Dofetilide (UK 68789)
    Dofetilide (UK 68789)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1671
    CAS #: 115256-11-6Purity ≥98%

    Description: Dofetilide (also known as UK-68789) is a potent and selective potassium channel (hERG) blocker, it is used as a Class III antiarrhythmic drug. Dofetilide blocks HERG currents in excised macro patches of Xenopus oocytes. 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. 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.

    References: J Cardiovasc Pharmacol. 1994 Oct;24(4):566-72; J Cardiovasc Pharmacol. 1996 Oct;28(4):576-84.

    Related CAS: 144449-71-8 (Dofetilide N-oxide; UK-116856); 1189700-56-8 (Dofetilide D4; UK 68789 D4)

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    Molecular Weight (MW)441.56
    FormulaC19H27N3O5S2
    CAS No.115256-11-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 88 mg/mL (199.3 mM)          
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Other info

    Chemical Name: N-(4-(2-(methyl(2-(4-(methylsulfonamido)phenoxy)ethyl)amino)ethyl)phenyl)methanesulfonamide

    InChi Key: IXTMWRCNAAVVAI-UHFFFAOYSA-N

    InChi Code: InChI=1S/C19H27N3O5S2/c1-22(13-12-16-4-6-17(7-5-16)20-28(2,23)24)14-15-27-19-10-8-18(9-11-19)21-29(3,25)26/h4-11,20-21H,12-15H2,1-3H3

    SMILES Code: CS(=O)(NC1=CC=C(OCCN(CCC2=CC=C(NS(=O)(C)=O)C=C2)C)C=C1)=O           

    SynonymsUK-68789; UK 68789; UK68789; Dofetilide; Dofetilidum; Tikosyn


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    In Vitro

    In vitro activity:  Dofetilide blocks HERG currents in excised macro patches of Xenopus oocytes. 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. 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.

    In VivoDofetilide (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. Dofetilide causes increased resorptions and the same stage-dependent malformations in Sprague-Dawley rats.
    Animal modelRats
    Formulation & Dosage100 mg/kg, i.v.
    References

    J Cardiovasc Pharmacol. 1994 Oct;24(4):566-72; J Cardiovasc Pharmacol. 1996 Oct;28(4):576-84.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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