Biological Information
Background Information:
The HERG potassium channel is a major molecular component of the delayed rectifier current (IKr) underlying cardiac repolarization. Due to either genetic defects in its pore-forming subunit or adverse drug effects, decreased HERG activity prolongs the QT interval and can lead to the potentially lethal ventricular arrhythmia Torsades de pointes. The implication of (IKr) in cardiac arrhythmias and in anti-arrhythmic/pro-arrhythmic actions of drugs has driven intensive research interests in its structure-function relationship, the linkage between LQT-associated mutations and changes in channel function, and the mechanism of drug actions.
Family:
Ion Channel
Sub Family:
Potassium
Class:
Voltage-Gated
Protein Name:
hERG
Uniprot Number:
Q12809
Protein Aliases:
Ether-a-go-go-related gene potassium channel 1|ERG-1|Eag-related protein 1|Ether-a-go-go-related protein 1|H-ERG|hERG-1|hERG1|Voltage-gated potassium channel subunit Kv11.1
Gene Name:
KCNH2
Gene ID:
3757
Gene Aliases:
Kv11.1|HERG|erg1
Accession Number:
NM_000238
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]Dofetilide
Ligand Kd (nM):
6.6
Ligand Concentration:
3 nM
Non Specific:
25 µM Terfenadine
Incubation:
60 min at RT
Control Inhibitor:
Terfenadine
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 μl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
2
Turnaround Time
Standard:
10 Business Days
Reference Compound Data
Additional Information
Brand:
SafetyScreen
Testing Location:
France - Celle L'Evescault
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