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• 产品描述： Ibutilide (U70226E) fumarate, an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells

• 靶点： Potassium Channel;CalciumChannel; SodiumChannel

• 体外研究：
  Ibutilide fumarate is a potent IKr blocker with an EC50 value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells. Ibutilide fumarate blocks IKr in cells expressing HERG+MDR1*1 to the same extent as cells expressing HERG alone (IC50: 22.5 nM vs 27.4 nM). However, cells expressing MDR1*7 show a marked resistance to Ibutilide (IC50: 105.3 nM vs 27.4 nM)

• 体内研究：
  Ibutilide fumarate prolongs cardiac repolarization in vitro and in vivo. Ibutilide (administered cumulatively in three doses, 0.01, 0.02 and 0.05 mg/kg i.v., each as a 10-min infusion) fumarate results in both polymorphic and monomorphic non-sustained ventricular tachycardia. Animal Model: Fifteen adult mongrel dogs of either sex Dosage: 0.01, 0.02 and 0.05 mg/kg Administration: Intravenous injection; each as a 10-min infusion Result: The action potential duration at 90% (APD90) prolongation with Ibutilide (0.01 mg/kg) was significantly greater in congestive heart failure (CHF) vs. controls.An increased dispersion of left-right ventricular APD90 was observed in CHF at 0.01 mg/kg, but not in controls.

• 参考文献：
  1. Ibutilide, a methanesulfonanilide antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells. Concentration-, time-, voltage-, and use-dependent effects. Circulation. 1995 Mar 15;91(6):1799-806. 2. B F McBride, et al. Influence of the G2677T/C3435T haplotype of MDR1 on P-glycoprotein trafficking and Ibutilide-induced block of HERG. Pharmacogenomics J. 2009 Jun;9(3):194-201. 3. S S Chugh, et al. Altered response to Ibutilide in a heart failure model. Cardiovasc Res. 2001 Jan;49(1):94-102.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.259 ml	11.297 ml	22.593 ml
  5 mM	0.452 ml	2.259 ml	4.519 ml
  10 mM	0.226 ml	1.13 ml	2.259 ml
  50 mM	0.045 ml	0.226 ml	0.452 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *