hERG Human Potassium Ion Channel [3H] Dofetilide Binding Antagonist Radioligand LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
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:
Full Length, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant potassium channel HERG expressed in human HEK-293 cells are used in modified Tris-HCl buffer pH 7.4. A 7.5 μg‡ aliquot is incubated with 3 nM [³H]Dofetilide for 60 minutes at 25°C. Non-specific binding is estimated in the presence of 10 μM Dofetilide. Channel proteins are filtered and washed, the filters are then counted to determine [³H]Dofetilide specifically bound. Compounds are screened at 10 μM.
Ligand:
[³H] Dofetilide
Ligand Kd (nM):
6.6
Ligand Concentration:
3 nM
Non Specific:
10 µM Dofetilide
Incubation:
60 min at 25°C
Control Inhibitor:
Dofetilide
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
10 Business Days
Express:
10 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Cardiovascular
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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