A2A Human Adenosine GPCR Cell Based Agonist & Antagonist cAMP LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
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). Adenosine A2A receptor agonism may cause hypotension, antagonism may facilitate platelet aggregation.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
A2A Human Adenosine GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
300500-0
Protein
A2A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
A2A Human Adenosine GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
Item
300500-1
Protein
A2A
Organism
Human
Assay Sub Type
Cell Based
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:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human adenosine A2A receptor-expressing HEK-293 cells are used. Test compound or vehicle is incubated with the cells in incubation buffer at 37°C for 10 minutes. The reaction is evaluated for cAMP levels by TR-FRET. Test compound-induced cAMP increase by 50 percent or more (≥50%) relative to the 0.1 μM NECA control response indicates possible adenosine A2A receptor agonist activity. Test compound-induced inhibition of the 3 nM NECA induced cAMP response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
10 min at 37°C
Control Inhibitor:
ZM 241385
Control Activator:
NECA
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
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
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