| Identification | Back Directory | [Name]
Ranolazine-d5 | [CAS]
1092804-87-9 | [Synonyms]
Ranolazine-d5
N-(2,6-dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl-1,1,2,3,3-d5]-1-piperazineacetamide | [Molecular Formula]
C24H28D5N3O4 | [MOL File]
1092804-87-9.mol | [Molecular Weight]
432.567 |
| Hazard Information | Back Directory | [Description]
Ranolazine-d5 is intended for use as an internal standard for the quantification of ranolazine by GC- or LC-MS. Ranolazine is a piperazine derivative with cardioprotective activity.1,2,3,4 It reduces the late sodium current (INa) in mouse myocytes expressing the long QT syndrome 3 mutant sodium channel DKPQ, ventricular myocytes isolated from a canine model of heart failure, guinea pig ventricular myocytes exposed to hydrogen peroxide or anemone toxin-II, and HEK293 cells expressing human Nav1.5 channels (IC50s = 5.9-15 μM) as well as the late potassium current (IKr) in canine ventricular myocytes and HEK293 cells (IC50s = 11.5 and 14.4 μM, respectively).1,2 Ranolazine also inhibits radioligand binding to α1-, β1-, and β2-adrenergic receptors (Kis = 8.2-19.5, 1.4-8.6, and 0.5-14.8 μM, respectively).2 In vivo, ranolazine (480 μg/kg per min) reduces clofilium-induced prolongation of the QTc interval and Torsade de Pointes (TdP) in rabbits.3 Ranolazine also reduces interstitial collagen deposition as well as atrial natriuretic peptide (ANP), connective tissue growth factor (CTGF), brain natriuretic peptide (BNP; ), and matrix metalloproteinase-2 (MMP-2) mRNA levels, and prevents left ventricular dilation in a mouse model of cardiotoxicity induced by doxorubicin .4 | [Uses]
Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent. | [References]
1. Shryock, J.C., and Belardinelli, L. Inhibition of late sodium current to reduce electrical and mechanical dysfunction of ischaemic myocardium Br. J. Pharmacol. 153(6),1128-1132(2008).
2. Verrier, R.L., Kumar, K., Nieminen, T., et al. Mechanisms of ranolazine’s dual protection against atrial and ventricular fibrillation Europace 15(3),317-324(2013).
3. Wang, W.Q., Robertson, C., Dhalla, A.K., et al. Antitorsadogenic effects of (±)-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine (ranolazine) in anesthetized rabbits J. Pharmacol. Exp. Ther. 325(3),875-881(2008).
4. Tocchetti, C.G., Carpi, A., Coppola, C., et al. Ranolazine protects from doxorubicin-induced oxidative stress and cardiac dysfunction Eur. J. Heart Fail. 16(4),358-366(2014). |
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