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. N-Type calcium channels are relatively insensitive to L-Type channel blockers and are specifically blocked with high affinity by peptide toxins from spiders and marine snails. The peptide toxins are potent blockers of synaptic transmission.

Family:

Ion Channel

Sub Family:

Calcium

Class:

Voltage-Gated

Protein Name:

Cav2.2 (N-type)

Uniprot Number:

Q00975 (human)

Gene Name:

CACNA1B

Gene ID:

774

Gene Aliases:

Cav2.2|CACNN

Organism:

Rat

Tissue:

Brain

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]omega -conotoxin GVIA

Ligand Kd (nM):

0.0007

Ligand Concentration:

0.001 nM

Non Specific:

10 nM Omega-conotoxin GVIA

Incubation:

30 min at RT

Control Inhibitor:

omega Cgtx

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

PubChem ID

4507

Name

Nitrendipine

Measurement

- IC50

PubChem ID

8378

Name

Neomycin

Measurement

370nM - IC50

PubChem ID

16132374

Name

omega Cgtx

Measurement

0.00162nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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