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

PubChem ID

2157

Name

Amiodarone

Measurement

220nM - IC50

PubChem ID

2247

Name

Astemizole

Measurement

1nM - IC50

PubChem ID

5405

Name

Terfenadine

Measurement

80nM - IC50

PubChem ID

159296

Name

Adenosine 3',5'-bisphosphate

Measurement

5nM - IC50

Additional Information

Brand:

SafetyScreen

Testing Location:

France - Celle L'Evescault

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