Dofetilide

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Chemical Structure| 115256-11-6 同义名 : UK 68789;Tikosyn;Dofetilidum;UK-68798
CAS号 : 115256-11-6
货号 : A253881
分子式 : C19H27N3O5S2
纯度 : 98%
分子量 : 441.565
MDL号 : MFCD00869707
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(237.79 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Potassium Channel
描述 Dofetilide is an antiarrhythmic drug that selectively inhibits the rapid component of the delayed rectifier potassium current. The administration of dofetilide may cause ventricular arrhythmias and torsade de pointes[3]. Dofetilide preferentially blocks open (or activated) channels and that the fast inactivation may competitively slow the binding kinetics. Dofetilide acts as a slow-onset/slow-offset open channel blocker of this current at nanomolar concentrations[4]. Dofetilide was found to be safe in patients after myocardial infarction and those with congestive heart failure and left ventricular systolic dysfunction (ejection fraction of less than 35%). Because dofetilide has about an 80% renal excretion, dose adjustment is required in patients with impaired renal function[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.32mL

2.26mL

1.13mL

22.65mL

4.53mL

2.26mL
参考文献

[1]Bauer A, Becker R, et al. Effects of the I(Kr)-blocking agent dofetilide and of the I(Ks)-blocking agent chromanol 293b on regional disparity of left ventricular repolarization in the intact canine heart. J Cardiovasc Pharmacol. 2002 Mar;39(3):460-7.

[2]Kiehn J, Lacerda AE, et al. Molecular physiology and pharmacology of HERG. Single-channel currents and block by dofetilide. Circulation. 1996 Nov 15;94(10):2572-9.

[3]Marcantoni I, Laratta R, Mascia G, et al. Dofetilide-Induced Microvolt T-Wave Alternans. Conf Proc IEEE Eng Med Biol Soc. 2019;2019:95-98

[4]Snyders DJ, Chaudhary A. High affinity open channel block by dofetilide of HERG expressed in a human cell line. Mol Pharmacol. 1996;49(6):949-955

[5]Shenasa F, Shenasa M. Dofetilide: Electrophysiologic Effect, Efficacy, and Safety in Patients with Cardiac Arrhythmias. Card Electrophysiol Clin. 2016;8(2):423-436