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Dofetilide(UK 68789)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dofetilide(UK 68789)图片
CAS NO:115256-11-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
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; Dofetilide; Dofetilidum; UK 68789; UK68789; Tikosyn
实验参考方法
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.