Biological Information
Background Information:
Nav1.5 is the predominant voltage-gated sodium channel expressed in cardiomyocytes and is encoded by the SCN5A gene. Structurally, Nav1.5 consists of a pore-forming α-subunit containing four homologous domains with six transmembrane segments each. It mediates the rapid inward sodium current responsible for depolarization of the cardiac action potential, playing a critical role in cardiac excitability and impulse conduction. Pathogenic variants in SCN5A can either increase or decrease Nav1.5 channel activity, disrupting cardiac electrical conduction and giving rise to a spectrum of inherited arrhythmia syndromes, including Long QT Syndrome, Brugada syndrome, sick sinus syndrome, and cardiac conduction disease. Due to its essential role in cardiac electrophysiology and safety pharmacology, Nav1.5 is a key target in cardiovascular risk assessment and drug discovery.
Family:
Ion Channel
Sub Family:
Sodium
Class:
Voltage-Gated
Protein Name:
Nav1.5
Uniprot Number:
Q14524
Protein Aliases:
Sodium channel protein type V subunit alpha; Voltage-gated sodium channel subunit alpha Nav1.5
Gene Name:
SCN5A
Gene ID:
6331
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
This assay measures the binding of [³H]BNZA to voltage-gated sodium channel Nav1.5. Human recombinant Nav1.5 expressed in CHO cells is used in modified Tris-HCl buffer pH 7.4. A 20 µg‡ aliquot of membrane is incubated with 1 nM [³H]BNZA for 180 minutes at 25℃. Non-specific binding is estimated in the presence of 100 µM Dibucaine. Membranes are filtered and washed 4 times, and the filters are counted to determine [³H]BNZA specifically bound. Compounds are screened at 10 µM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.
Ligand:
[³H]BNZA
Ligand Kd (nM):
11
Ligand Concentration:
1 nM
Non Specific:
100 µM Dibucaine
Incubation:
180 min at 25°C
Control Inhibitor:
Dibucaine
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
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Cardiovascular
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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