CB2 Human Cannabinoid GPCR Binding Agonist Radioligand LeadHunter Assay - FR

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Cannabinoid receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Cannabinoid CB2 receptors are found primarily in immune tissues.

Family:

GPCR

Sub Family:

Cannabinoid

Class:

Class A

Protein Name:

CB2

Uniprot Number:

P34972

Protein Aliases:

CB2|hCB2|CX5

Gene Name:

CNR2

Gene ID:

1269

Gene Aliases:

CB2

Accession Number:

NM_001841

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]WIN 55212-2

Ligand Kd (nM):

1.5

Ligand Concentration:

0.8 nM

Non Specific:

5 µM WIN 55212-2

Incubation:

120 min at 37°C

Control Inhibitor:

Win-55212-2

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:

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

5281969

Name

Anandamide

Measurement

470nM - IC50

PubChem ID

5311501

Name

Win-55212-2

Measurement

1.5nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

Cannabinoid CB2 receptor agonism may limit angiogenesis as well as induce apoptosis in some types of cancer, inhibit inflammatory pain and the immune system. CB2 receptor antagonism may facilitate mast cell-mediated allergic and inflammatory responses.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault