130656-51-8

130656-51-8 structure

Name: Nifekalant hydrochloride
Chemical Name: Nifekalant Hydrochloride
CAS Number: 130656-51-8
Molecular Formula: C₁₉H₂₈ClN₅O₅
Molecular Weight: 441.90900
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
Create Date: 2018-09-12 11:00:37
Modify Date: 2024-01-06 07:11:42
Nifekalant hydrochloride (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC50 of 10 µM. Nifekalant hydrochloride can be used for refractory ventricular tachyarrhythmias research[1][2].

Name	Nifekalant Hydrochloride
Synonyms	MFCD00892243 Nifekalant hydrochloride 6-[2-[2-hydroxyethyl-[3-(4-nitrophenyl)propyl]amino]ethylamino]-1,3-dimethylpyrimidine-2,4-dione,hydrochloride

Description	Nifekalant hydrochloride (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC50 of 10 µM. Nifekalant hydrochloride can be used for refractory ventricular tachyarrhythmias research[1][2].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel
In Vitro	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].
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].
References	[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.

Boiling Point	597.9ºC at 760mmHg
Molecular Formula	C₁₉H₂₈ClN₅O₅
Molecular Weight	441.90900
Flash Point	315.4ºC
Exact Mass	441.17800
PSA	125.32000
LogP	1.72940
Storage condition	2-8°C

130656-51-8	130636-43-0
1406-14-0	6138-79-0
127228-87-9	143851-98-3
929-73-7	65546-09-0
1135280-78-2	56-99-5