Biological Information

Background Information:

Adenosine 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. Adenosine receptors may also be called P1 receptors, which are distinguished from transmitter-gated ion channels (P2X receptors) and G protein-coupled receptors (P2Y).

Family:

GPCR

Sub Family:

Adenosine

Class:

Class A

Protein Name:

A2A

Uniprot Number:

P29274

Gene Name:

ADRA2A

Gene ID:

135

Gene Aliases:

RDC8|ADORA2

Accession Number:

NM_000675

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]CGS 21680

Ligand Kd (nM):

27

Ligand Concentration:

6 nM

Non Specific:

10 µM NECA

Incubation:

120 min at RT

Control Inhibitor:

NECA

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

1329

Name

8-Cyclopentyl-1,3-dipropylxanthine

Measurement

40nM - IC50

PubChem ID

448222

Name

NECA

Measurement

28nM - IC50

PubChem ID

3086599

Name

Cgs 21680

Measurement

55nM - IC50

PubChem ID

Name

CPA

Measurement

1500nM - iC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

Adenosine A2A receptor agonism may cause hypotension; antagonism may facilitate platelet aggregation.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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