Ranolazine dihydrochloride
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Ranolazine dihydrochloride
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CAS No:
95635-56-6
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Formula:
C24H35Cl2N3O4
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Chemical Name:
Ranolazine dihydrochloride
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Synonyms:
(+/-)-4-[2-HYDROXY-3-(O-METHOXYPHENOXY)PROPYL]-1-PIPERAZINEACETO-2',6'-XYLIDIDE DIHYDROCHLORIDE;n-(2,6-dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]acetamide dihydrochloride;(+/-)-N-(2,6-DIMETHYLPHENYL)-4-[2-HYDROXY-3-(2-METHOXYPHENOXY)PROPYL]-1-PIPERAZINEACETAMIDE DIHYDROCHLORIDE;RANOLAZINE DIHYDROCHLORIDE;RANOLAZINE HCL;Ranolazine DiHCI;Ranolazine and salt;N-(2,6-Dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)-propyl)piperazin-1-yl)acetamide di
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CAS No:
Description
Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP). IC50 value:Target: sodium-dependent calcium channelRanolazine is currently approved for use in chronic angina. The basis for this use is likely related to inhibition of late sodium channels with resultant beneficial downstream effects. Randomiz
An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.
Ranolazine is a piperazine derivative with cardioprotective activity. 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). 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).In vivo, ranolazine (480 μg/kg per min) reduces clofilium-induced prolongation of the QTc interval and Torsade de Pointes (TdP) in rabbits. Ranolazine also reduces interstitial collagen deposition as well as atrial natriuretic peptide (ANP; Item Nos.24539|24276), 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 .
White Crystalline Powder
Characteristics
74.3
3.86080
off-white solid
222-229.5 °C(lit.)
624.1ºC at 760 mmHg
331.2ºC
H2O: soluble ≥10mg/mL
Desiccate at RT
Desiccate at RT
Safety Information
NONH for all modes of transport
3
22-24/25
TK7845370
Desiccate at RT
|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.
Drug Information
A class of drugs that act by inhibition of sodium influx through cell membranes. Blockade of sodium channels slows the rate and amplitude of initial rapid depolarization, reduces cell excitability, and reduces conduction velocity. (See all compounds classified as Sodium Channel Blockers.)|Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume. (See all compounds classified as Cardiovascular Agents.)
43285, RS
Ranolazine dihydrochloride Use and Manufacturing
treatment of angina and congestive heart failure
Ranolazine Dihydrochloride is an anti-ischemic agent which modulates myocardial metabolism. Antianginal.
Computed Properties
Molecular Weight:500.5
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:9
Exact Mass:499.2004620
Monoisotopic Mass:499.2004620
Topological Polar Surface Area:74.3
Heavy Atom Count:33
Complexity:531
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes
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