Nifekalant
Nifekalant Basic information
- Product Name:
- Nifekalant
- Synonyms:
-
- NIFEKALANT
- NIFEKALANT HCL
- 6-[2-[2-hydroxyethyl-[3-(4-nitrophenyl)propyl]amino]ethylamino]-1,3-dimethyl-pyrimidine-2,4-dione
- 6-((2-((2-hydroxyethyl)(3-(p-nitrophenyl)propyl)amino)ethyl)amino)-1,3-dimethyl-uracil
- 1,3-dimethyl-6-[2-(n-(2-hydroxyethyl)-3-(4-nitrophenyl)propylamino)ethylamino]-2,4(1h,3h)-pyrimidinedione hydrochloride
- NIFEKALANT [6-((2-((2-HYDROXYETHYL)(3-(P-NITROPHENYL)PROPYL)AMINO)ETHYL)AMINO)-1,3-DIMETHYL-URACIL]
- 6-[2-[2-hydroxyethyl-[3-(4-nitrophenyl)propyl]amino]ethylamino]-1,3-dimethyl-pyrimidine-2,4-quinone
- OEBPANQZQGQPHF-UHFFFAOYSA-N
- CAS:
- 130636-43-0
- MF:
- C19H27N5O5
- MW:
- 405.45
- Product Categories:
-
- API
- Mol File:
- 130636-43-0.mol
Nifekalant Chemical Properties
- Melting point:
- 117.5-118.5°; mp 125-126° (Katakami, 1992)
- Boiling point:
- 597.9±60.0 °C(Predicted)
- Density
- 1.32±0.1 g/cm3(Predicted)
- pka
- 14.74±0.10(Predicted)
- CAS DataBase Reference
- 130636-43-0(CAS DataBase Reference)
Nifekalant Usage And Synthesis
Uses
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].
Definition
ChEBI: Nifekalant is an amine.
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. DOI:10.1016/j.bmcl.2004.06.070
[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. DOI:10.4330/wjc.v3.i6.169
[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. DOI:10.1111/j.1476-5381.1996.tb15762.x
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