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 A2B receptor agonism may cause vascular and intestinal smooth muscle relaxation, antagonism may be useful in the treatment of pulmonary inflammation associated with asthma.

Family:

GPCR

Sub Family:

Adenosine

Class:

Class A

Protein Name:

A2B

Uniprot Number:

P29275

Gene Name:

ADORA2B

Gene ID:

136

Accession Number:

XM_017024197

Organism:

Human

Construct Details:

Recombinant

Cell Type:

HEK293

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:

XAC

Control Activator:

NECA (1000 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 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

1329

Name

8-Cyclopentyl-1,3-dipropylxanthine

Measurement

860nM - IC50

PubChem ID

2690

Name

CGS-15943

Measurement

47nM - IC50

PubChem ID

6603931

Name

MRS 1754

Measurement

5000nM - IC50

PubChem ID

Name

XAC

Measurement

110nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

Adenosine A2B receptor agonism may cause vascular and intestinal smooth muscle relaxation, antagonism may be useful in the treatment of pulmonary inflammation associated with asthma.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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