Nifekalant

CAS: 130636-43-0 F: C19H27N5O5 W: 405.45

Nifekalant (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC50 of 10 μM. Nifeka

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Bioactivity	Nifekalant (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC50 of 10 μM. Nifekalant can be used for refractory ventricular tachyarrhythmias research[1][2].
Invitro	Nifekalant interacts with the cardiac M2 and the peripheral M3 receptors with a Ki value of 27 and 74 mM, respectively. Nifekalant dose dependently blocks HERG channels with an IC50 value of 7.9 mM, but Nifekalant does not block minK currents in the Xenopus oocyte expression system. Nifekalant blocks HERG channels mainly in their open state in a frequency dependent manner. As a pure K+ channel blocker, Nifekalant does not have negative inotropic effects which amiodarone has via a β-blocking action and does not affect cardiac conduction[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Nifekalant 相关抗体:
In Vivo	In rats (a species deficient in functional cardiac IK), before coronary ligation, 3 mg/kg and 10 mg/kg MS-551 decreased the heart rate by 6% and 12%, and increased mean arterial pressure (MAP) by 14% and 33%, respectively. MS-551 prolongs the QT interval and reduced the incidence of sustained ventricular fibrillation (VF) after reperfusion[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
CAS	130636-43-0
Formula	C19H27N5O5
Molar Mass	405.45
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Lü-Pei Du, et al. The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4771-7. [2]. Ioannis N Pantazopoulos, et al. Nifekalant in the treatment of life-threatening ventricular tachyarrhythmias. World J Cardiol. 2011 Jun 26;3(6):169-76. [3]. J Chen, et al. IK independent class III actions of MS-551 compared with sematilide and dofetilide during reperfusion in anaesthetized rats. Br J Pharmacol. 1996 Nov;119(5):937-42.