Flecainide acetate
(Synonyms: 氟卡胺; R-818) 目录号 : GC15823
An inhibitor of cardiac late sodium current
Cas No.:54143-56-5
Sample solution is provided at 25 µL, 10mM.
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Flecainide, a nonselective Na (+) channel blocker, is a class 1C antiarrhythmic drug, especially used for the management of supraventricular arrhythmia. Flecainide has been used extensively in the effect on providing long-term sinus rhythm (SR) restoration as well as decreasing AF symptoms.
Flecainide revealed to suppress the Nav1.5 sodium channel in the heart, leading to prolongation of the cardiac action potential. Flecainide showed to reduce Ca+ spark, wave frequency and Ca+ wave velocity in the intact rat cardiomyocyte. Besides, flecainide has shown to reduce Ca(2+) wave when I(Na) is active. It has been demonstrated that flecainide could remarkably increase the Na(+)/Ca(2+)-exchanger (NCX)-mediated Ca(2+) efflux [1].
Flecainide has been reported to prolong ventricular repolarization, with the stronger effect at the left ventricular epicardium related to the right ventricular epicardium. Flecainide was found to produce a greater effective refractory period (ERP) lengthening at endocardium than epicardium, leading to a significant increase of ERP dispersion across the ventricular wall [2].
Flecainide has shown to dose-dependently reduce systemic pressures (32% at 0.8 μg/mL) and peripheral vascular resistance (15% at 0.8 μg/mL). In addition, at therapeutic plasma concentrations, flecainide at 0.8 μg/mL remarkably reduced the heart rate (55 beats/min) and increased QRS intervals (9.9 msec) in a rat hindlimb perfusion model [3].
References:
1.Sikkel MB1, Collins TP, Rowlands C, Shah M, O'Gara P, Williams AJ, Harding SE, Lyon AR, MacLeod KT. Flecainide reduces Ca(2+) spark and wave frequency via inhibition of the sarcolemmal sodium current. Cardiovasc Res. 2013 May 1;98(2):286-96. doi: 10.1093/cvr/cvt012. Epub 2013 Jan 19.
2.Osadchii OE.Flecainide-induced proarrhythmia is attributed to abnormal changes in repolarization and refractoriness in perfused guinea-pig heart. J Cardiovasc Pharmacol. 2012 Nov;60(5):456-66. doi: 10.1097/FJC.0b013e31826b86cf.
3.Allison B1, Yang Y, Pourrier M, Gibson JK. Comparison of the in vivo hemodynamic effects of the antiarrhythmic agents vernakalant and flecainide in a rat hindlimb perfusion model. J Cardiovasc Pharmacol. 2011 Apr;57(4):463-8. doi: 10.1097/FJC.0b013e318210276b.
| Cas No. | 54143-56-5 | SDF | |
| 别名 | 氟卡胺; R-818 | ||
| 化学名 | acetic acid;N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide | ||
| Canonical SMILES | CC(=O)O.C1CCNC(C1)CNC(=O)C2=C(C=CC(=C2)OCC(F)(F)F)OCC(F)(F)F | ||
| 分子式 | C19H24F6N2O5 | 分子量 | 474.39 |
| 溶解度 | ≥ 47.4mg/mL in DMSO, ≥ 47.4mg/mL in EtOH, ≥ 23.7mg/mL in Water with ultrasonic and warming | 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 | 2.108 mL | 10.5399 mL | 21.0797 mL |
| 5 mM | 0.4216 mL | 2.108 mL | 4.2159 mL |
| 10 mM | 0.2108 mL | 1.054 mL | 2.108 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet