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Nicainoprol

Cat. No. M30584
Nicainoprol Structure
Synonym:

RU-42924

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Biological Activity

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

Chemical Information
Molecular Weight 369.46
Formula C21H27N3O3
CAS Number 76252-06-7
Form Solid
Solubility (25°C) DMSO ≥ 29 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] P A Martorana, et al. Eur J Pharmacol. 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

[2] C C Libersa, et al. Eur Heart J. Electrophysiological effects of intravenous nicaïnoprol, a new antiarrhythmic agent, in 11 patients

[3] K Hashimoto, et al. Jpn J Pharmacol. Antiarrhythmic effect of a new class 1 antiarrhythmic drug, nicainoprol, on canine ventricular arrhythmias

[4] T Kimura, et al. J Cardiovasc Pharmacol. Electrophysiologic effects of nicainoprol, a putative class I antiarrhythmic agent, on the guinea pig ventricular papillary muscle

[5] J Weirich, et al. J Cardiovasc Pharmacol. Evaluation and interpretation of voltage- and frequency-dependent electrophysiologic effects of a new class I antiarrhythmic agent (nicainoprol) on guinea pig papillary muscle and isolated heart

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Keywords: Nicainoprol, RU-42924 supplier, Sodium Channel, inhibitors, activators


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