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

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

10 min at 37°C

Control Inhibitor:

AM 630

Control Activator:

WIN 55,212-2 mesylate (3 nM)

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 finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

4302962

Name

AM 281

Measurement

1514nM - IC50

PubChem ID

4302963

Name

AM 630

Measurement

529nM - IC50

PubChem ID

11113928

Name

AM 251

Measurement

1083nM - 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

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