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Nicainoprol (RU-42924)

Catalog No.GC31216

Nicainoprol (RU-42924) is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.

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Nicainoprol (RU-42924) Chemical Structure

Cas No.: 76252-06-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$488.00
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1mg
$144.00
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5mg
$600.00
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Sample solution is provided at 25 µL, 10mM.

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Background

Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.

The antiarrhythmic agent Nicainoprol, a fast-sodium-channel blocking drug, also protected isolated rat hearts against reperfusion arrhythmias, but is without beneficial effects on cardiac hemodynamics and biochemical parameters, in contrast to the ACE inhibitor[1].

The effect of the novel antiarrhythmic agent Nicainoprol on coronary occlusion and reperfusion arrhythmia is investigated in isolated working rat hearts and in anesthetized rats. In isolated working rat hearts Nicainoprol (10 μM, 5 μM and 100 μM) induces concentration-related protection against reperfusion arrhythmia without changing the cardiodynamics, with the exception of a decrease in heart rate at the highest concentration. Enzyme levels (lactate dehydrogenase and creatine kinase) in the coronary venous effluent, and cardiac tissue concentrations of glycogen, lactate, ATP and creatine phosphate are not affected by Nicainoprol. Given to anesthetized rats, Nicainoprol (5 and 10 mg/kg i.v.) reduces dose dependently in the early post occlusion (0-30 min) period, the percentage of animals with premature ventricular complexes (PVCs) and ventricular tachycardia while completely preventing the occurrence of ventricular fibrillation. In the reperfusion period no animal treated with 5 mg/kg and 12% of the rats treated with 10 mg/kg showed PVCs (the only form of arrhythmia observed in this period) versus 60% of the control rats. Both doses of Nicainoprol induces a decrease in heart rate, blood pressure and myocardial oxygen consumption. The ratio of infarct mass to ventricular mass is significantly reduced by 20% at a dose of 5 mg/kg and by 28% at the dose of 10 mg/kg. Nicainoprol could be useful in the prevention and treatment of arrhythmias associated with acute myocardial infarction[2].

[1]. Linz W, et al. Cardiac arrhythmias are ameliorated by local inhibition of angiotensin formation and bradykinin degradation with the converting-enzyme inhibitor ramipril. Cardiovasc Drugs Ther. 1989 Dec;3(6):873-82. [2]. Martorana PA, et al. Effects of nicainoprol on reperfusion arrhythmia in the isolated working rat heart and on ischemia and reperfusion arrhythmia and myocardial infarct size in the anesthetized rat. Eur J Pharmacol. 1987 Nov 17;143(3):391-401.

Chemical Properties

Cas No. 76252-06-7 SDF
Canonical SMILES O=C(N1CCCC2=C1C(OCC(O)CNC(C)C)=CC=C2)C3=CC=CN=C3
Formula C21H27N3O3 M.Wt 369.46
Solubility DMSO : ≥ 29 mg/mL (78.49 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.7067 mL 13.5333 mL 27.0665 mL
5 mM 0.5413 mL 2.7067 mL 5.4133 mL
10 mM 0.2707 mL 1.3533 mL 2.7067 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 32 reference(s) in Google Scholar.)

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