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Eleclazine (hydrochloride)

Product NameEleclazine (hydrochloride)
CAS1448754-43-5
MFC21H17ClF3N3O3
MW451.83
EINECS
MOL File1448754-43-5.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMSO:100.0(Max Conc. mg/mL);221.32(Max Conc. mM)
form	Solid
color	White to off-white
InChI	InChI=1S/C21H16F3N3O3.ClH/c22-21(23,24)30-16-5-2-14(3-6-16)15-4-7-18-17(12-15)20(28)27(10-11-29-18)13-19-25-8-1-9-26-19;/h1-9,12H,10-11,13H2;1H
InChIKey	ZRYHNOXHGYUHFF-UHFFFAOYSA-N
SMILES	O=C1N(CCOC2=CC=C(C3C=CC(OC(F)(F)F)=CC=3)C=C12)CC1=NC=CC=N1.Cl

Usage And Synthesis

Uses

Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 value of <1 μM and approximately 14.2 μM, respectively. Eleclazine hydrochloride shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine hydrochloride can be used to research cardiac arrhythmias[1][2][3].

in vivo

Eleclazine (0.3 and 0.9 mg/kg; IV; infused over 15 minutes) reduces the incidence of epinephrine-induced ventricular premature beats and couplets, and shortens ventricular QT and atrial PTa intervals^[1].

Animal Model:	Male Yorkshire pigs (35.20 ± 0.46 kg; injected with epinephrine via a jugular vein)^[1]
Dosage:	0.3 and 0.9 mg/kg
Administration:	IV; infused over 15 minutes
Result:	Reduced the incidence of epinephrine-induced ventricular premature beats and couplets by 51% (from 31.3 ± 1.91 to 15.2 ± 5.08 episodes; P = 0.038) and the incidence of 3- to 7-beat ventricular tachycardia (VT) by 56% (from 10.8 ± 3.45 to 4.7 ± 3.12 episodes; P = 0.004). Shortened ventricular QT and atrial PTa intervals by 7%, and reduced atrial repolarization alternans and heterogeneity without attenuation of the inotropic response to catecholamine.

References

[1] Bacic D, et al. 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. Heart Rhythm. 2017 Mar;14(3):448-454. DOI:10.1016/j.hrthm.2016.10.021
[2] Rajamani S et al. The novel late Na+ current inhibitor, GS-6615 (eleclazine) and its anti-arrhythmic effects in rabbit isolated heart preparations. Br J Pharmacol. 2016 Jul 23. DOI:10.1111/bph.13563
[3] Potet F, Egecioglu DE, Burridge PW, George AL Jr. GS-967 and Eleclazine Block Sodium Channels in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes. Mol Pharmacol. 2020 Nov;98(5):540-547. DOI:10.1124/molpharm.120.000048

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