IBUTILIDE
Names
Biological Activity
[Description]:
Ibutilide (U70226E free base), an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells[1].
[Related Catalog]:
[In Vitro]
Ibutilide is a potent IKr blocker with EC50 value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells[1]. Ibutilide blocks IKr in cells expressing HERG+MDR1*1 to the same extent as cells expressing HERG alone (IC50: 22.5±0.9 vs 27.4±2.5 nM). However, cells expressing MDR1*7 show a marked resistance to Ibutilide (IC50: 105.3±1.42 nM vs 27.4±2.5 nM)[2].
[In Vivo]
Ibutilide prolongs cardiac repolarization in vitro and in vivo[1]. Ibutilide infusions (administered cumulatively in three doses, 0.01, 0.02 and 0.05 mg/kg i.v., each as a 10-min infusion) results in both polymorphic and monomorphic non-sustained ventricular tachycardia[3]. Animal Model: Fifteen adult mongrel dogs of either sex[1] Dosage: 0.01, 0.02 and 0.05 mg/kg Administration: 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.
[References]
Chemical & Physical Properties
[ Density]:
1.099g/cm3
[ Boiling Point ]:
522.4ºC at 760mmHg
[ Molecular Formula ]:
C20H36N2O3S
[ Molecular Weight ]:
384.57600
[ Flash Point ]:
269.7ºC
[ Exact Mass ]:
384.24500
[ PSA ]:
78.02000
[ LogP ]:
5.31780
[ Vapour Pressure ]:
9.71E-12mmHg at 25°C
[ Storage condition ]:
2-8°C
Safety Information
[ Hazard Codes ]:
Xn
[ Risk Phrases ]:
R22