A2B Human Adenosine GPCR Binding Antagonist Radioligand LeadHunter Assay - FR
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:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]CPX
Ligand Kd (nM):
65
Ligand Concentration:
5 nM
Non Specific:
100 µM NECA
Incubation:
60 min at RT
Control Inhibitor:
NECA
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:
2
Turnaround Time
Standard:
10 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:
France - Celle L'Evescault
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