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:

ADORA2A

Gene ID:

135

Gene Aliases:

RDC8|ADORA2

Accession Number:

NM_000675

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

10 min at 37°C

Control Inhibitor:

ZM 241385

Criteria For Significance:

≥ 50% Increase in cAMP relative to NECA response, ≥ 50% Inhibition of NECA-induced cAMP increase

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

16

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

176407

Name

ZM241385

Measurement

7.7nM - 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:

Taiwan - Taipei

RELATED SOLUTIONS

Item: 300500
Item: 300500-0
Item: 200610