ELECLAZINE HYDROCHLORIDE

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 Search

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

Molecular Formula	C21H16F3N3O3
Molecular Weight	415.3652
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://adisinsight.springer.com/drugs/800037785 | https://www.ncbi.nlm.nih.gov/pubmed/27690427

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 Target	Pharmacology	Condition	Potency
Sodium channel protein type V alpha subunit 49 Target ID: CHEMBL1980 Sources: https://www.ncbi.nlm.nih.gov/pubmed/29017927	Blocker 537		0.97 µM [IC50]

PubMed

Title	Date	PubMed

Patents

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

Substance Class	Chemical Created by `admin` on `Sat Dec 16 00:26:34 GMT 2023` Edited by `admin` on `Sat Dec 16 00:26:34 GMT 2023`
Record UNII	4R1JP3Q4HI
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ELECLAZINE HYDROCHLORIDE

Common Name

English

1,4-BENZOXAZEPIN-5(2H)-ONE, 3,4-DIHYDRO-4-(2-PYRIMIDINYLMETHYL)-7-(4-(TRIFLUOROMETHOXY)PHENYL)-, HYDROCHLORIDE (1:1)

Systematic Name

English

Eleclazine hydrochloride [WHO-DD]

Common Name

English

Code System Code Type Description

PUBCHEM

90479986