产品说明书

Ibutilide fumarate

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Chemical Structure| 122647-32-9 同义名 : U70226E;(±)-Ibutilide (hemifumarate);Ibutilide fumarate, Corvert, Ibutilida, Ibutilidum
CAS号 : 122647-32-9
货号 : A179082
分子式 : C44H76N4O10S2
纯度 : 99%+
分子量 : 885.225
MDL号 : MFCD01715410
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(56.48 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(56.48 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Sodium Channel
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... 展开 >>nd Sudden Death 收起 << Phase 2 Completed - United States, Indiana ... 展开 >> Indiana Clinical Research Center Indianapolis, Indiana, United States, 46202 Purdue University Indianapolis, Indiana, United States, 46202 收起 <<
NCT01929083 - Completed - -
NCT02513940 Prolonged QT Interval in EKG a... 展开 >>nd Sudden Death 收起 << Phase 4 Completed - United States, Indiana ... 展开 >> Indiana University Indianapolis, Indiana, United States, 46202 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.13mL

0.23mL

0.11mL

5.65mL

1.13mL

0.56mL

11.30mL

2.26mL

1.13mL
参考文献

[1]Bickford CL, Agarwal R, et al. Efficacy and safety of ibutilide for chemical cardioversion of atrial fibrillation and atrial flutter in cancer patients. Am J Med Sci. 2014 Apr;347(4):277-81.

[2]Sun JL, Han R, et al. Effects of ibutilide on canine cardiac pacing threshold and on induction rates of atrial fibrillation. Cell Biochem Biophys. 2012 Dec;64(3):197-203.

[3]Kodirov SA, Zhuravlev VL, Brachmann J. Prevailing Effects of Ibutilide on Fast Delayed Rectifier K+ Channel. J Membr Biol. 2019;252(6):609‐616

[4]Howard PA. Ibutilide: an antiarrhythmic agent for the treatment of atrial fibrillation or flutter. Ann Pharmacother. 1999; 33(1):38‐47

[5]Foster RH, Wilde MI, Markham A. Ibutilide. A review of its pharmacological properties and clinical potential in the acute management of atrial flutter and fibrillation. Drugs. 1997; 54(2):312‐330

[6]Nair M, George LK, Koshy SK. Safety and efficacy of ibutilide in cardioversion of atrial flutter and fibrillation. J Am Board Fam Med. 2011; 24(1):86‐92