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CAS No.: 748810-28-8

Vernakalant HCl/盐酸维那卡兰 Catalog No. CSN12970

Synonyms: RSD1235 hydrochloride;RSD1235 HCl;RSD-1235

Vernakalant HCl prolongs repolarization by blocking atrial potassium channels, it's a class III antiarrhythmics.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Potassium Channel Kv1.5 (I508F)

IC50:0.61±0.03μM Potassium Channel Kv1.5 (T479A)

IC50:1.63±0.09μM Potassium Channel Kv1.5

IC50:13.35±0.93μM
描述Kv1.5 underlies the ultrarapid delayed rectifier outward K⁺ currents that are observed naturally in atrium of heart, whereas they appear to be absent from ventricle. Kv1.5 play an important role in determining the length of cardiac action potentials and, therefore, have been the targets of antiarrhythmic drugs ^[3]. Vernakalant, a mixed voltage- and frequency-dependent Na⁺ and atria-preferred K⁺ channel blocker, is used to convert atrial fibrillation rapidly and safely in patients. Block by vernakalant of Kv1.5 wild type and mutants was assessed in transiently transfected human embryonic kidney 293 cells. The IC₅₀ values were 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel^wt, Kv1.5 channel^I508F, Kv1.5 channel^T479A, respectively. In the presence of 10 μM vernakalant, rapid block was apparent after channel opening, and a steady-state currentlevel was rapidly reached. Upon repolarization, the tail current amplitude was initially less than in control, but decayed more slowly and crossed over the control tracing as it declined to thebaseline current level suggesting that vernakalant delayed closing of Kv1.5 ^[4].
作用机制Ile502 in the S6 domain is a key residue in the block of Kv1.5 by vernakalant ^[4].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT00989001 Atrial Fibrillation Phase 3 Terminated - -
NCT01174160 Atrial Fibrillation Phase 3 Completed - -
NCT01174160 - - Completed - -
更多
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00989001	Atrial Fibrillation	Phase 3	Terminated	-	-
NCT01174160	Atrial Fibrillation	Phase 3	Completed	-	-
NCT01174160	-	-	Completed	-	-

[1] Chiba T, Kondo N, et al. Influences of rapid pacing-induced electrical remodeling on pharmacological manipulation of the atrial refractoriness in rabbits. J Pharmacol Sci. 2016 Mar;130(3):170-6.
[2] Eldstrom J, Wang Z,et al. The molecular basis of high-affinity binding of the antiarrhythmic compound vernakalant (RSD1235) to Kv1.5 channels. Mol Pharmacol. 2007 Dec;72(6):1522-34.
[3] Lee HM, Hahn SJ, Choi BH. Blockade of Kv1.5 by paroxetine, an antidepressant drug. Korean J Physiol Pharmacol. 2016 Jan;20(1):75-82. doi: 10.4196/kjpp.2016.20.1.75. Epub 2015 Dec 31. PMID: 26807026; PMCID: PMC4722194.
[4] Eldstrom J, Wang Z, Xu H, Pourrier M, Ezrin A, Gibson K, Fedida D. The molecular basis of high-affinity binding of the antiarrhythmic compound vernakalant (RSD1235) to Kv1.5 channels. Mol Pharmacol. 2007 Dec;72(6):1522-34. doi: 10.1124/mol.107.039388. Epub 2007 Sep 14. PMID: 17872968.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5912 mL
- 12.9559 mL
- 25.9117 mL
- 5 mM
- 0.5182 mL
- 2.5912 mL
- 5.1823 mL
- 10 mM
- 0.2591 mL
- 1.2956 mL
- 2.5912 mL

技术信息

CAS号

748810-28-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H32ClNO4

运输

蓝冰

分子量

385.93

别名

RSD1235 hydrochloride;RSD1235 HCl;RSD-1235;Vernakalant HCl;Kynapid;Brinavess;盐酸维那卡兰

溶解度

DMSO	50.0 mg/mL (129.6 mM) warming

动物实验配方

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靶点	Description	IC50
Potassium Channel Kv1.5 (I508F)		IC50:0.61±0.03μM
Potassium Channel Kv1.5 (T479A)		IC50:1.63±0.09μM
Potassium Channel Kv1.5		IC50:13.35±0.93μM

Vernakalant HCl/盐酸维那卡兰 Catalog No. CSN12970

靶点选择性

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