Nifekalant (hydrochloride)
(Synonyms: 盐酸尼非卡兰,MS-551) 目录号 : GC44403
A class III antiarrhythmic agent
Cas No.:130656-51-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nifekalant is a class III antiarrhythmic agent that has been shown to be beneficial to initial resuscitation after cardiac arrest in clinical trials. It blocks the rapidly activating delayed rectifier potassium channel (IKr; IC50 = 10 µM). Nifekalant is also inhibits the human multidrug and toxin extrusion (MATE) transporter 1 (MATE1; IC50 = 6.5 µM).
| Cas No. | 130656-51-8 | SDF | |
| 别名 | 盐酸尼非卡兰,MS-551 | ||
| Canonical SMILES | OCCN(CCNC1=CC(N(C)C(N1C)=O)=O)CCCC2=CC=C([N+]([O-])=O)C=C2.Cl | ||
| 分子式 | C19H27N5O5•HCl | 分子量 | 441.9 |
| 溶解度 | DMSO : 125 mg/mL (282.86 mM; ultrasonic and warming and heat to 60°C) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.263 mL | 11.3148 mL | 22.6296 mL |
| 5 mM | 0.4526 mL | 2.263 mL | 4.5259 mL |
| 10 mM | 0.2263 mL | 1.1315 mL | 2.263 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。
Efficacy of Nifekalant hydrochloride in the treatment of fatal ventricular arrhythmia in patients with ischemic heart disease
Int Heart J 2005 Jul;46(4):647-56.PMID:16157956DOI:10.1536/ihj.46.647.
Ventricular tachycardia (VT), which causes hemodynamic instability, and ventricular fibrillation (VF) sometimes occur in patients with severe underlying cardiovascular disease such as myocardial ischemia or infarction, and are associated with high mortality. This report presents the efficacy of Nifekalant hydrochloride (Nifekalant), a pure class III antiarrhythmic agent, in treating life-threatening ventricular arrhythmia in such patients. From June 2000, when Nifekalant became commercially available in Japan, to May 2003, 30 ischemic heart disease (IHD) patients with VT/VF resistant to direct-current (DC) countershock received Nifekalant in our hospital. These 30 patients served as the Nifekalant group in this study. As a control group, we also included 33 IHD patients with VT/VF that had been resistant to DC countershock upon or during hospitalization between January 1996 and May 2000 before Nifekalant became commercially available. No significant differences were observed in patient background factors and treatments between the two groups. The rates of death within 48 hours of occurrence of VT/VF were significantly lower in the Nifekalant group (7%, 2/30) than in the control group (27%, 9/33; P < 0.03). The rates of cardiac death during hospitalization were also significantly lower in the Nifekalant group (40%, 12/30) than in the control group (67%, 22/33; P < 0.03). The rates of survival until hospital discharge were significantly higher in the Nifekalant group (57%, 17/30) than in the control group (30%, 10/33; P < 0.03). Multivariate analysis of all 63 patients revealed Nifekalant administration was the factor that significantly improved the mortality (odds ratio for cardiac death, 0.26; 95% confidence interval (CI), 0.07 to 0.95; P = 0.041). Nifekalant improves the prognosis for life-threatening ventricular arrhythmia in IHD patients.
Nifekalant hydrochloride and Amiodarone hydrochloride Result in Similar Improvements for 24-Hour Survival in Cardiopulmonary Arrest Patients: The SOS-KANTO 2012 Study
J Cardiovasc Pharmacol 2015 Dec;66(6):600-9.PMID:26317166DOI:10.1097/FJC.0000000000000310.
Background: Amiodarone (AMD), Nifekalant (NIF), and lidocaine (LID) hydrochlorides are widely used for ventricular tachycardia/fibrillation (VT/VF). This study retrospectively investigated the NIF potency and the differential effects of 2 initial AMD doses (≤150 mg or 300 mg) in the Japanese SOS-KANTO 2012 study population. Methods and results: From 16,164 out-of-hospital cardiac arrest cases, 500 adult patients using a single antiarrhythmic drug for shock-resistant VT/VF were enrolled and categorized into 4 groups (73 LID, 47 NIF, 173 AMD-≤150, and 207 AMD-300). Multivariate analyses evaluated the outcomes of NIF, AMD-≤150, or AMD-300 groups versus LID group. Odds ratios (ORs) for survival to admission were 3.21 [95% confidence interval (CI): 1.38-7.44, P < 0.01] in NIF and 3.09 (95% CI: 1.55-6.16, P < 0.01) in AMD-≤150 groups and significantly higher than those of the LID group. However, the OR was 1.78 (95% CI: 0.90-3.51, P = 0.10) in AMD-300 group and was not significant than LID group. ORs for 24-hour survival were 6.68 in NIF, 4.86 in AMD-≤150, and 2.97 in AMD-300, being significantly higher in these groups. Conclusions: NIF and AMD result in similar improvements for 24-hour survival in cardiopulmonary arrest patients, and this suggest the necessity of a randomized control study.
An HPLC method for the determination of Nifekalant hydrochloride in canine plasma and its application to a pharmacokinetic study
J Chromatogr Sci 2013 Oct;51(9):867-71.PMID:23169932DOI:10.1093/chromsci/bms182.
In this study, a simple and selective high-performance liquid chromatography method was developed and validated for the determination of Nifekalant hydrochloride in canine plasma. Liquid-liquid extraction was used to separate Nifekalant hydrochloride from canine plasma and the mean extraction recoveries of Nifekalant hydrochloride and the internal standard were 82.31 and 94.81%, respectively. The chromatographic separation was performed on a Dikma Diamonsil column with a mobile phase consisting of acetonitrile-20mM phosphate buffer (pH 6.2; 30:70, v/v) with flow rate of 1.0 mL/min. The standard curve was linear over the concentration range of 20-10,000 ng/mL (r(2) > 0.99). The intra-batch and inter-batch accuracy for Nifekalant hydrochloride at four concentrations were 93.14-100.47% and 96.12-103.77%, respectively. The relative standard deviations were less than 15%. The method was successfully applied to a pharmacokinetic study after the intravenous administration of Nifekalant hydrochloride to beagle dogs.
Anti-arrhythmic efficacy of Nifekalant hydrochloride, a pure class III anti-arrhythmic agent, in patients with healed myocardial infarction and inducible sustained ventricular tachycardia
J Cardiovasc Pharmacol 2002 Nov;40(5):735-42.PMID:12409982DOI:10.1097/00005344-200211000-00011.
In recent clinical trials, class III anti-arrhythmic drugs were found to reduce arrhythmic deaths in patients after myocardial infarction. The purpose of this study was to assess the electrophysiologic properties and anti-arrhythmic efficacy for inducible sustained ventricular tachycardias (VTs) of the pure class III agent Nifekalant hydrochloride (MS-551) in comparison with those of procainamide. Programmed ventricular stimulation of up to three extra stimuli was performed for induction of VTs. Effective refractory period (ERP) of the ischemic zone and normal zone was also measured before and after Nifekalant. Nifekalant and procainamide suppressed sustained VT induction in four of 15 patients and in six of 15 patients, respectively (p = NS). Sinus cycle length, PR interval, and QRS duration were not changed, but QT and QTc intervals were significantly increased with Nifekalant (p < 0.01). Ventricular ERP also increased, whereas there were no significant differences in the increase of ERP between the ischemic and normal zones. The suppression of VT induction did not correlate with the changes in QT, QTc, and ERP after Nifekalant administration. There were no significant differences in induced VT cycle length at baseline study between responders and nonresponders to Nifekalant. Reverse use dependence was not apparent on review of electrophysiologic parameters. Neither proarrhythmic events nor hemodynamic disturbances occurred after Nifekalant administration. It was concluded that Nifekalant could be used safely and showed comparable effectiveness to procainamide for the suppression of VT induction.
Nifekalant in the treatment of life-threatening ventricular tachyarrhythmias
World J Cardiol 2011 Jun 26;3(6):169-76.PMID:21772943DOI:10.4330/wjc.v3.i6.169.
The aim of the present study is to review the literature and discuss Nifekalant's potential use as a first aid drug in an emergency care setting. The PubMed database was used to identify papers, using keywords Nifekalant, MS-551, amiodarone and lidocaine. Nifekalant hydrochloride, formally known as MS-551, is a class III antiarrhythmic agent which acts only by increasing the time course of myocardial repolarization. It was developed and is currently being used only in Japan for the treatment of ventricular tachyarrhythmias. It is a non-selective K(+) channel blocker without any β-blocking actions. Administration of Nifekalant suppressed sustained ventricular tachyarrhythmias in acute coronary syndrome patients, and in cardiac arrest victims as well as during or after cardiac surgery. The major adverse effect of Nifekalant is QT interval prolongation and occurrence of torsades de pointes which requires frequent monitoring of the QT interval during Nifekalant infusion with adequate dose adjustment. Nifekalant is a possible effective antiarrhythmic agent for refractory ventricular tachyarrhythmias. Further clinical studies are required before Nifekalant is routinely used in the emergency care setting.