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Eleclazine

Cat. No. M22297
Eleclazine Structure
Synonym:

GS-6615

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Biological Activity

Eleclazine

Chemical Information
Molecular Weight 415.37
Formula C21H16F3N3O3
CAS Number 1443211-72-0
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] Franck Potet, et al. Mol Pharmacol. GS-967 and Eleclazine Block Sodium Channels in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes

[2] Rachel E Caves, et al. Heart Rhythm O2. Inhibition of voltage-gated Na+ currents by eleclazine in rat atrial and ventricular myocytes

[3] Nesrine El-Bizri, et al. Heart Rhythm. Eleclazine exhibits enhanced selectivity for long QT syndrome type 3-associated late Na+ current

[4] Danilo Bacic, et al. Heart Rhythm. Eleclazine, an inhibitor of the cardiac late sodium current, is superior to flecainide in suppressing catecholamine-induced ventricular tachycardia and T-wave alternans in an intact porcine model

[5] Henrique Fuller, et al. Heart Rhythm. Eleclazine, a new selective cardiac late sodium current inhibitor, confers concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in an intact porcine model

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