General
Preferred name
VERNAKALANT
Synonyms
RSD1235 ()
RSD1235 hydrochloride ()
VERNAKALANT HYDROCHLORIDE ()
Vernakalant (Hydrochloride) ()
MK-6621 ()
Vernakalant (RSD1235) Hydrochloride ()
Vernakalant hcl ()
Brinavess ()
Kynapid ()
RSD-1235 ()
P&D ID
PD071822
CAS
748810-28-8
605683-48-5
794466-70-9
Tags
available
drug
Approved by
EMA
First approval
2010
Drug indication
Atrial fibrillation
Drug Status
approved
investigational
Max Phase
4.0
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
Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35¡À0.93 ¦ÌM, 0.61¡À0.03 ¦ÌM, and 1.63¡À0.09 ¦ÌM for Kv1.5 channelwt, Kv1.5 channelI508F, Kv1.5 channelT479A, respectively.
PRICE
238
MOA
Vernakalant blocks atrial voltage-gated sodium channels in a dose and frequency-dependent manner and inhibits late sodium current (INa)which confers its effect on intra-atrial conduction. This current blockade enhance and onset of drug action accelerates in higher heart rate as the affinity of vernakalant for INa also increases. Its binding offset is quick once the heart rate slows [A19198]. It also blocks Kv 1.5 channel and its early activating potassium channels (IKur) and inhibits acetylcholine-activated potassium channels (IKAch), which are specific to the atrium and cause prolongation of atrial refractoriness. Vernakalant also blocks Kv4.3 channel and its cardiac transient outward potassium current (Ito), which is involved more with atrial than ventricular refractoriness [A19203]. ; Vernakalant minimally blocks hERG channels and its rapidly activating/delayed rectifying potassium current (IKr) which accounts for mild QT prolongation. QRS widening due to INa blockade also contributes to QT prolongation [A19197].
DESCRIPTION
Vernakalant Hydrochloride (RSD1235 hydrochloride) is a mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blocker.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
12
ChEMBL Approved Drugs
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
43
Molecular Weight
349.23
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
1
cLogP
2.64
TPSA
51.16
Fraction CSP3
0.7
Chiral centers
3.0
Largest ring
6.0
QED
0.82
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Potassium Channel
KV1.5 channel
Sodium Channel
KCNA5
Potassium Channel,Sodium Channel
Pathway
Membrane Transporter/Ion Channel
Indication
atrial fibrillation (AF)
MOA
potassium channel blocker
Source data
