hERG Binding Assay Services
GenScript's hERG binding assay services utilize [3H]Dofetilide to detect the binding level of compound and hERG channel directly. With ample expertise on scintillation proximity assay (SPA) and filtration binding assay, GenScript can offer flexible high throughput screening (HTS) solutions for hERG screening. Coupling ExpressPatch hERG Testing Service, GenScript guarantee your fast and reliable data for validating hERG blockers.
Assay Setup Showcases
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Name: hERG channel
Source: Human recombinant (HEK293 cells)
Radioligand: [3H]Dofetilide (3.6 nM)
Membrane Preparation: 10 μg/well
Bmax: 3 pmol/mg protein
Kd: 3.6 nM
Binding Buffer: 10 mM HEPES, NaCl 130 mM, KCl 60 mM, 0.8 mM MgCl2, 1mM NaEGTA, 10 mM glucose, 0.1% BSA (pH 7.4)
Wash Buffer: 10 mM Tris-HCl, pH 7.4
Incubation: 37°C, 60 min
Detection Technique: Filtration
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Table 1. Ki/IC50 (nM)of Reference Compounds on hERG
Compound |
[3H]Dofetilide Competition (Ki) |
GenScript Patch Clamp (IC50) |
GenScript |
Reference |
Manual |
QPatch 16 |
Astemizole |
3 |
1±0 |
35 |
15 |
Dofetilide |
6 |
40±010 |
N/A |
56 |
Cisapride |
28 |
80±030 |
21 |
56 |
Terfenadine |
115 |
30±010 |
46 |
133 |
Haloperidol |
144 |
90±010 |
66 |
50 |
Verapamil |
208 |
990±110 |
146 |
618 |
Quinidine |
2997 |
1310±280 |
1560 |
985 |
Aspirin |
N/A |
N/A |
> 1,000,000 |
> 1,000,000 |
Reference:
Finlayson, K., L. Turnbull, 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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Quotations and Ordering:
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Our customer service representatives are available 24 hours a day, Monday through Friday to assist you.
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Email: bioassay@genscript.com |
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Phone: 1-877-436-7274 (Toll-Free) 1-732-885-9188 |
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Fax: 1-732-210-0262 1-732-885-5878 |
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