General
Preferred name
LUF7244
Synonyms
P&D ID
PD055142
CAS
1821638-43-0
Tags
available
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
LUF7244 is a selective allosteric modulator of Kv11.1 channels. LUF7244 inhibits early afterdepolarizations. LUF7244 can be used for anti-arrhythmia research[1].
DESCRIPTION
LUF7244 is a negative allosteric modulator (NAM) of orthosteric ligand binding to the hERG channel (Kv11.1) . It was used to test the hypothesis that hERG NAMs might be able to counteract the proarrhythmic effects of hERG-blocking drugs. Using as a known hERG orthosteric channel blocker, LUF7244 has been shown to protect against dofetilideāinduced early after depolarizations (EADs) in vitro and dofetilideāinduced TdP arrhythmia in vivo . It has been proposed that hERG NAMs might find therapeutic potential to alleviate long QTs caused by hERG-blocking drugs, and/or to treat patients with congential long QT syndromes that are associated with Kv11.1 and Kv7.1 channels.
(GtoPdb)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
3
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
7
Molecular Weight
366.08
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
6
Ring Count
3
Aromatic Ring Count
3
cLogP
3.98
TPSA
68.29
Fraction CSP3
0.05
Chiral centers
0.0
Largest ring
6.0
QED
0.67
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Kv11.1 channel NAM
Potassium Channel
Pathway
Membrane Transporter/Ion Channel
Source data

