Dofetilide

目录号: GC17152纯度: >98.00%同义词: 多非利特; UK 68789

An antiarrythmic agent that inhibits potassium channels

Cas No.: 115256-11-6

规格	价格	库存	数量	操作
10mg	¥462.00	现货	1
10mM (in 1mL DMSO)	¥452.00	现货	1

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187(9):2288-2304 (2024)
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183(7):1867-1883 (2020)
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产品描述 Description

Dofetilide(Tikosyn) is a class III antiarrhythmic agent.Target: Potassium ChannelIn patients with congestive heart failure and reduced left ventricular function, dofetilide was effective in converting atrial fibrillation, preventing its recurrence, and reducing the risk of hospitalization for worsening heart failure. Dofetilide had no effect on mortality [1]. 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 [2].

References:
[1]. Maisch, B., et al., [Pregnancy and cardiomyopathies]. Herz, 2003. 28(3): p. 196-208.
[2]. Snyders, D.J. and A. Chaudhary, High affinity open channel block by dofetilide of HERG expressed in a human cell line. Mol Pharmacol, 1996. 49(6): p. 949-55.

实验参考方法 Experimental Reference Method

Cell experiment [1,2]:
Cell lines	HEK293 cells, guinea pig cardiomyocytes
Preparation method	The solubility of this compound in DMSO is >21.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	1 μM
Applications	In a human cell line and human embryonic kidney 293 transfected with HERG, dofetilide induced channel block with the EC50 of 12 ± 2 nM. Induction of block depended on depolarization beyond the threshold for channel opening. Dofetilide acted as a slow-onset/slow-offset open channel blocker of this current at nanomolar concentrations. Dofetilide (1 μM) reduced 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.
Animal experiment [3]:
Animal models	Dogs with old myocardial infarction (MI)
Dosage form	Intravenous injection, 100 mg/kg
Application	Dofetilide (100 mg/kg, i.v.) suppressed the reentry arrhythmia induced by PES in dogs with old myocardial infarction (MI). Dofetilide showed antiarrhythmic effect in some dogs with digitalis arrhythmia. Dofetilide increased QT interval and showed negative chronotropic effect.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1]. Snyders D J, Chaudhary A. High affinity open channel block by dofetilide of HERG expressed in a human cell line[J]. Molecular Pharmacology, 1996, 49(6): 949-955. [2]. Kiehn J, Villena P, Beyer T, et al. Differential effects of the new class III agent dofetilide on potassium currents in guinea pig cardiomyocytes[J]. Journal of cardiovascular pharmacology, 1994, 24(4): 566-572. [3]. Chen J, Xue Y, Eto K, et al. Effects of dofetilide, a class III antiarrhythmic drug, on various ventricular arrhythmias in dogs[J]. Journal of cardiovascular pharmacology, 1996, 28(4): 576-584.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号

115256-11-6

同义词

多非利特; UK 68789

化学名

N-[4-[2-[2-[4-(methanesulfonamido)phenoxy]ethyl-methylamino]ethyl]phenyl]methanesulfonamide

SMILES

CN(CCC1=CC=C(C=C1)NS(=O)(=O)C)CCOC2=CC=C(C=C2)NS(=O)(=O)C

分子式

C₁₉H₂₇N₃O₅S₂

分子量

441.56 g/mol

溶解性

≥ 21.15mg/mL in DMSO

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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