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Details

Stereochemistry ACHIRAL
Molecular Formula C21H16F3N3O3.ClH
Molecular Weight 451.826
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ELECLAZINE HYDROCHLORIDE

SMILES

Cl.FC(F)(F)OC1=CC=C(C=C1)C2=CC3=C(OCCN(CC4=NC=CC=N4)C3=O)C=C2

InChI

InChIKey=ZRYHNOXHGYUHFF-UHFFFAOYSA-N
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

HIDE SMILES / InChI

Description

Eleclazine (formerly known as GS-6615) is a dihydrobenzoxazepinone selective cardiac late sodium current inhibitor. Gilead Sciences is developing eleclazine as an oral treatment for long QT syndrome, hypertrophic cardiomyopathy, ischaemic heart disease, and Ventricular arrhythmias.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
0.97 µM [IC50]

PubMed

Sample Use Guides

In Vivo Use Guide
Phase 3 clinical trial designed to determine the efficacy, safety, and tolerability of the late sodium current inhibitor eleclazine in shortening the corrected QT (QTcF) interval in subjects with type 3 Long QT Syndrome (LQT3). 41 subjects with genotype-confirmed LQT3 received a 48 mg oral loading dose of eleclazine followed by 12 weeks of treatment with 3 mg oral eleclazine once daily and then 12 weeks of treatment with 6 mg oral eleclazine once daily.
Route of Administration: Oral