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 (L-type)

Uniprot Number:

Q13936

Gene Name:

CACNA1C

Gene ID:

775

Gene Aliases:

Cav1.2|CACH2|CACN2|TS|LQT8

Accession Number:

NM_000719

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetry

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human calcium channel Cav1.2 expressing HEK293 cells are seeded and incubated at 37°C with 5% CO₂ overnight. After incubation with the Fluo-4 direct dye for 1 hour, the test compound or vehicle with 25 mM KCl is added and incubated for 20 minutes at RT. Fluorescence intensity is measured before and after the addition of the KCl-containing incubation buffer, resulting in a final concentration of 80 mM KCl. Inhibition of the fluorescence response by the test compound is calculated relative to the potassium-induced response, with 1 µM Isradipine defined as 100% inhibition. An inhibition of 50 percent or more (≥50%) indicates calcium channel Cav1.2 inhibition activity.

Incubation:

20 min at RT

Control Inhibitor:

Isradipine

Criteria For Significance:

≥ 50% inhibition in fluorescence relative to KCl-induced response

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

120 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

16

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

3784

Name

Isradipine

Measurement

0.53nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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