Biological Information

Background Information:

Sodium channels are the founding members of the superfamily of ion channels that include voltage-gated potassium and calcium channels. Unlike the different classes of potassium and calcium channels, however, the functional properties of the known sodium channels (NaV) are relatively similar. Voltage-gated Sodium Site 2 channels, found in central neurons primarily localized to unmyelinated and pre-myelinated axons, govern action, potential initiation, and repetitive firing. Consequently, antagonists may be antiepileptic and antiarrhythmic as well as proarrhythmic; agonists may also cause cardiac arrhythmia. Nav1.5 is the isoform related to cardiovascular toxicity and is recommended for safety pharmacology profiling.

Family:

Ion Channel

Sub Family:

Sodium

Class:

Voltage-Gated

Protein Name:

Nav1.5

Uniprot Number:

Q14524 (human)

Protein Aliases:

Sodium channel protein cardiac muscle subunit alpha,Sodium channel protein type V subunit alpha,Voltage-gated sodium channel subunit alpha Nav1.5

Gene Name:

SCN5A

Gene ID:

6331

Gene Aliases:

HB1; HB2; HH1; IVF; VF1; HBBD; ICCD; LQT3; SSS1; CDCD2; CMD1E; CMPD2; PFHB1; Nav1.5

Organism:

Human

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

MS

Testing Information

Ligand:

Batrachotoxin

Ligand Kd (nM):

27.5nM

Ligand Concentration:

15 nM

Non Specific:

Terfenadine, 10 µM

Incubation:

360 min at 22°C

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

2247

Name

Astemizole

Measurement

61nM - IC50

PubChem ID

5405

Name

Terfenadine

Measurement

57nM - IC50

PubChem ID

6280

Name

Vératridine

Measurement

24 000nM - IC50

PubChem ID

16219577

Name

Lidocaine

Measurement

100 000nM - IC50

PubChem ID

71183216

Name

Eleclazine

Measurement

1200nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: P447
Item: P456