General
Preferred name
ELECLAZINE
Synonyms
GS 6615 hydrochloride ()
GS-6615 ()
Eleclazine (hydrochloride) ()
GS 6615 (hydrochloride) ()
Eleclazine hydrochloride ()
Eleclazina ()
P&D ID
PD048623
CAS
1443211-72-0
1448754-43-5
Tags
available
drug candidate
Drug indication
hypertrophic cardiomyopathy
Long QT syndrome
Ischemic heart disease
Drug Status
investigational
Max Phase
3.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Eleclazine is a sodium channel inhibitor, modulating cardiac late Na+ currents via the Nav1.5 (gene symbol SCN5A) channel. The compound is a dihydrobenzodiazepine type structure. Dihydrobenzodiazepine scaffolds are being developed as α-helix mimetics, with the potential to inhibit protein-protein interactions . This chemical structure and its use is covered by patent US20150038489 .
(GtoPdb)
DESCRIPTION
Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 value of <1 ¦ÌM and approximately 14.2 ¦ÌM, 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].
PRICE
166
DESCRIPTION
Eleclazine hydrochloride (GS 6615 hydrochloride) is a novel inhibitor of late Na+ current (IC50: 0.7 uM).
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
11
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
26
Molecular Weight
415.11
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
0
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
4.08
TPSA
64.55
Fraction CSP3
0.19
Chiral centers
0.0
Largest ring
7.0
QED
0.64
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Na+ current
Sodium Channel
Potassium Channel
Member status
member
MOA
Nav1.5 channel inhibitor
late sodium current inhibitor
Pathway
Membrane Transporter/Ion Channel
Source data
