| Product Name |
Human Kv11.1 (HERG) Channel Membrane Preparation |
Species |
Human |
| Documents |
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 Document-EXAMPLE: 11908_20100223002708.JPG (JPG) |
| Document-EXAMPLE: 11909_20100223002738.JPG (JPG) |
| TECHNICAL MANUAL: 11910_20100223014803.PDF (PDF) |
| Figures |
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| Reference |
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Diaz G. et. al. (2004) The [3H]dofetilide binding assay is a predictive screening tool for hERG blockade and proarrhythmia: Comparison of intact cell and membrane preparations and effects of altering [K+]o. J. Pharmacol. Toxicol. Methods. 50(3):187-99.
Chen, M. et al. (2007). Improved functional expression of recombinant human ether-a-go-go (hERG) K+ channels by cultivation at reduced temperature. BMC. Biotechnol. 7: 93.
Finlayson, K. et al. (2001). [3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen. Eur. J. Pharmacol. 430(1): 147-8.
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Description |
hERG (human ether-a-go-go related gene) codes for a protein known as Kv11.1 potassium ion channel. This ion channel mediates the repolarizing IKr current in the cardiac action potential. Suppression of IKr by loss of function mutations in the hERG gene or by untoward drug block can prolong the QT interval and predispose patients to the potentially lethal arrhythmia Torsades de Pointes (TdP). A number of clinically drugs in the market have had the tendency to inhibit hERG, which can increase concomitant risk of sudden death as well as cause other side effects. Therefore, hERG channel is an important antitarget to avoid during drug development. |
Host Cell |
HEK293/hERG |
Concentration |
1 mg/ml in 50 mM HEPES, 0.1 mM EDTA, 10 % glycerol |
Storage |
Store at -80°C |
Quality Control |
Bmax and Kd are determined using radioligand saturation binding assays (Figure 1).
Expression Level (Bmax): 2.61 pmol/mg membrane protein.
Kd for [3H]Dofetilide: 3.57 nM
|
Application |
Binding assay for human Kv11.1 (hERG) channel |
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Document-EXAMPLE: 11908_20100223002708.JPG (JPG)
Document-EXAMPLE: 11909_20100223002738.JPG (JPG)