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多非利特 /Dofetilide {[allProObj[0].p_purity_real_show]}

货号:A253881 同义名: UK 68789;Tikosyn Ambeed 开学季,买赠积分,赢豪礼

Dofetilide is a potassium channel blocker that acts as a class III antiarrhythmic drug. It is used for the treatment of atrial fibrillation and flutter.

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Dofetilide 化学结构 CAS号:115256-11-6
Dofetilide 化学结构
CAS号:115256-11-6
Dofetilide 3D分子结构
CAS号:115256-11-6
Dofetilide 化学结构 CAS号:115256-11-6
Dofetilide 3D分子结构 CAS号:115256-11-6
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Dofetilide 纯度/质量文件 产品仅供科研

货号:A253881 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Potassium Channel 其他靶点 纯度
Tolbutamide {[allProObj[0].p_purity_real_show]}
Glimepiride ++++

SUR1, IC50: 5.4 nM

SUR2B, IC50: 7.3 nM

{[allProObj[0].p_purity_real_show]}
Dronedarone Hydrochloride {[allProObj[0].p_purity_real_show]}
Gliquidone ++

Potassium channel, IC50: 27.2 nM

{[allProObj[0].p_purity_real_show]}
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

{[allProObj[0].p_purity_real_show]}
Glibenclamide {[allProObj[0].p_purity_real_show]}
Amiodarone HCl {[allProObj[0].p_purity_real_show]}
Gliclazide ++

Potassium channel, IC50: 184 nM

{[allProObj[0].p_purity_real_show]}
Repaglinide {[allProObj[0].p_purity_real_show]}
Dofetilide {[allProObj[0].p_purity_real_show]}
Nateglinide {[allProObj[0].p_purity_real_show]}
Quinine hydrochloride dihydrate {[allProObj[0].p_purity_real_show]}
ML133 HCl +

Kir2.1, IC50: 290 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Dofetilide 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].

Dofetilide 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

Dofetilide 实验方案

计算器
存储液制备 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

Dofetilide 技术信息

CAS号115256-11-6
分子式C19H27N3O5S2
分子量 441.565
别名 UK 68789;Tikosyn;Dofetilidum;UK-68798
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -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
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