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CAS No.: 122647-32-9

Ibutilide fumarate/富马酸伊布利特 Catalog No. CSN11184

Synonyms: U70226E;(±)-Ibutilide (hemifumarate);Corvert

Ibutilide Fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm.

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生物活性

描述Ibutilide fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm. Ibutilide at concentrations ranging between 10 nM and 100 µM inhibited IKr (rectifier potassium currents) in dose-dependent manner with a half maximal effective concentration of 2.03 ± 0.74 µM (n = 5-10). The amplitude of tail currents activated by prepulse to + 20 mV was decreased from 253 ± 52 to 130 ± 25 pA (n = 8, p < 0.01) in the presence of 1 µM ibutilide. The slow IKs persisted to greater extent even at 100 μM ibutilide revealing a distinguishable selectivity toward the IKr component^[3]. Ibutilide is a Vaughan-Williams class III antiarrhythmic agent approved for intravenous use for the rapid termination of recent-onset AF or AFl (atrial fibrillation or atrial flutter). The drug is extensively metabolized by the liver, has a volume of distribution of 11 - 15 L/kg, is 40% protein bound, and has an elimination half-life of 6 hours in patients^[4]. Intravenous ibutilide 0.01 to 0.025 mg/kg or 1 to 2 mg successfully converted atrial flutter or fibrillation to sinus rhythm in 33 to 49% of patients in 2 placebo-controlled trials involving 439 patients with sustained arrhythmia^[5]. Ibutilide is also safe and efficient in the treatment of atrial fibrillation in patients who have had cardiac surgery, and in accessory pathway-mediated atrial fibrillation Where the conversion rate of ibutilide is as high as 95%^[6].
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
NCT01929083	Prolonged QT Interval in EKG a... more >>nd Sudden Death Collapse <<	Phase 2	Completed	-	United States, Indiana ... more >> Indiana Clinical Research Center Indianapolis, Indiana, United States, 46202 Purdue University Indianapolis, Indiana, United States, 46202 Collapse <<
NCT01929083	-	-	Completed	-	-
NCT02513940	Prolonged QT Interval in EKG a... more >>nd Sudden Death Collapse <<	Phase 4	Completed	-	United States, Indiana ... more >> Indiana University Indianapolis, Indiana, United States, 46202 Collapse <<

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参考文献

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
- 1.1297 mL
- 5.6483 mL
- 11.2966 mL
- 5 mM
- 0.2259 mL
- 1.1297 mL
- 2.2593 mL
- 10 mM
- 0.1130 mL
- 0.5648 mL
- 1.1297 mL

技术信息

CAS号

122647-32-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C44H76N4O10S2

运输

蓝冰

分子量

885.23

别名

U70226E;(±)-Ibutilide (hemifumarate);Corvert;Ibutilida;Ibutilidum;富马酸伊布利特

溶解度

DMSO	176.0 mg/mL (198.8 mM)
Ethanol	176.0 mg/mL (198.8 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01929083	Prolonged QT Interval in EKG a... more >>nd Sudden Death Collapse <<	Phase 2	Completed	-	United States, Indiana ... more >> Indiana Clinical Research Center Indianapolis, Indiana, United States, 46202 Purdue University Indianapolis, Indiana, United States, 46202 Collapse <<
NCT01929083	-	-	Completed	-	-
NCT02513940	Prolonged QT Interval in EKG a... more >>nd Sudden Death Collapse <<	Phase 4	Completed	-	United States, Indiana ... more >> Indiana University Indianapolis, Indiana, United States, 46202 Collapse <<
NCT03370536	Atrial Fibrillation ... more >> Persistent Atrial Fibrillation Collapse <<	Not Applicable	Terminated(1 patient enrolled ... more >>(consented) but screen failed. Study stopped as unable to enroll.) Collapse <<	-	United States, New York ... more >> Icahn School of Medicine at Mount Sinai New York, New York, United States, 10029 Collapse <<
NCT01014741	Persistent Atrial Fibrillation	Not Applicable	Completed	-	United States, California ... more >> Regional Cardiology Associates Sacramento, California, United States, 95823 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 United States, New York Icahn School of Medicine at Mount Sinai New York, New York, United States, 10029 United States, Virginia University Of Virginia Health System Charlottesville, Virginia, United States, 22908 Canada, Ontario Sunnybrook Health Sciences Centre Toronto, Ontario, Canada, M4N 3M5 Korea, Republic of Republic of Korea University Medical Center Seoul, Korea, Republic of Collapse <<
NCT01447862	Atrial Fibrillation	Phase 4	Completed	-	Austria ... more >> Medical University of Vienna, Department of Emergency Medicine Vienna, Austria, A-1090 Collapse <<
NCT01014741	-	-	Completed	-	-
NCT00589992	Atrial Fibrillation ... more >> Pulmonary Vein Ablation Collapse <<	Not Applicable	Unknown	December 2016	United States, Indiana ... more >> Medical Consultants, P.C. Recruiting Muncie, Indiana, United States, 47303 Contact: Sherry Adair, RN 765-254-4761 skadair@medicalconsultantspc.com Principal Investigator: Antonio Navarrete, MD Collapse <<

Ibutilide fumarate/富马酸伊布利特 Catalog No. CSN11184

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