Cav1.2 (L-type) Rat Calcium Ion Channel Binding (Dihydropyridine Site) LeadHunter Assay - FR
OVERVIEW
DOCUMENTS/REFERENCES
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 (DHP 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]nitrendipine
Ligand Kd (nM):
0.27
Ligand Concentration:
0.25 nM
Non Specific:
1 µM Nitrendipine
Incubation:
90 min at RT
Control Inhibitor:
Nitrendipine
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:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Cardiovascular
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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