Biological Information

Background Information:

Voltage-gated calcium channels mediate calcium influx in response to membrane depolarization and regulate intracellular processes such as contraction, secretion, neurotransmission, and gene expression. They are members of a gene superfamily of transmembrane ion channel proteins that includes voltage-gated potassium and sodium channels. Pharmacology of the three families of calcium channels is quite distinct. Cav1.2, L-Type calcium channel blockers are used in the therapy of cardiovascular disease.

Family:

Ion Channel

Sub Family:

Calcium

Class:

Voltage-Gated

Protein Name:

CaV1.2 (Vera. site)

Uniprot Number:

Q13936 /Q08289/P54289 (human)

Gene Name:

CACNA1C/CACNB2/CACNA2D1

Gene ID:

775/783/781

Organism:

Rat

Tissue:

Brain

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]D888

Ligand Kd (nM):

3

Ligand Concentration:

3 nM

Non Specific:

10 µM D 600

Incubation:

120 min at RT

Control Inhibitor:

Gallopamil

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

1234

Name

Gallopamil

Measurement

24nM - IC50

PubChem ID

2520

Name

Verapamil

Measurement

39nM - IC50

PubChem ID

4507

Name

Nitrendipine

Measurement

1.2nM - IC50

PubChem ID

39186

Name

Diltiazem

Measurement

240nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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