Dofetilide
(Synonyms: 多非利特; UK 68789) 目录号 : GC17152
An antiarrythmic agent that inhibits potassium channels
Cas No.:115256-11-6
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1,2]: | |
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Cell lines |
HEK293 cells, guinea pig cardiomyocytes |
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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. |
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Reacting condition |
1 μM |
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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]: | |
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Animal models |
Dogs with old myocardial infarction (MI) |
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Dosage form |
Intravenous injection, 100 mg/kg |
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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. |
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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. |
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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. | |
| Cas No. | 115256-11-6 | SDF | |
| 别名 | 多非利特; UK 68789 | ||
| 化学名 | N-[4-[2-[2-[4-(methanesulfonamido)phenoxy]ethyl-methylamino]ethyl]phenyl]methanesulfonamide | ||
| Canonical 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 |
| 溶解度 | ≥ 21.15mg/mL in DMSO | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2647 mL | 11.3235 mL | 22.647 mL |
| 5 mM | 0.4529 mL | 2.2647 mL | 4.5294 mL |
| 10 mM | 0.2265 mL | 1.1323 mL | 2.2647 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet