A2B Human Adenosine GPCR Binding Antagonist Radioligand 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 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
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant adenosine A2B receptors expressed in human HEK-293 cells are used in modified Tris-HCl buffer pH 6.5. A 6 μg‡ aliquot is incubated with 1.6 nM [³H]MRS1754 for 90 minutes at 25°C. Non-specific binding is estimated in the presence of 100 μM NECA. Receptors are filtered and washed, the filters are then counted to determine [³H]MRS1754 specifically bound. Compounds are screened at 10 μM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.
Ligand:
[³H] MRS1754
Ligand Kd (nM):
0.77
Ligand Concentration:
1.6 nM
Non Specific:
100 µM NECA
Incubation:
90 min at 25°C
Control Inhibitor:
8-Cyclopentyl-1,3-dipropylxanthine
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
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:
Taiwan - Taipei
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