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:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

30 min at 37°C

Control Inhibitor:

8-Cyclopentyl-1,3-dipropylxanthine

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

1329

Name

8-Cyclopentyl-1,3-dipropylxanthine

Measurement

0.2μM -

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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