A3 Human Adenosine GPCR Binding Agonist Radioligand LeadHunter Assay - FR

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Adenosine receptors belong to the superfamily of G-protein coupled receptors and contain 7 transmembrane domains. Four major subtypes of the adenosine receptor have been termed A1, A2A, A2B and A3. A3 receptors are found in high levels in the testis, and in lower levels in the lung, kidney, heart, and CNS.

Family:

GPCR

Sub Family:

Adenosine

Class:

Class A

Protein Name:

Uniprot Number:

P0DMS8

Gene Name:

ADORA3

Gene ID:

140

Gene Aliases:

AD026

Accession Number:

NM_000677|NM_020683

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]AB-MECA

Ligand Kd (nM):

0.22

Ligand Concentration:

0.15 nM

Non Specific:

1 µM IB-MECA

Incubation:

120 min at RT

Control Inhibitor:

IB-MECA

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:

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

1329

Name

8-Cyclopentyl-1,3-dipropylxanthine

Measurement

3000nM - IC50

PubChem ID

123683

Name

IB-MECA

Measurement

0.27nM - IC50

PubChem ID

448222

Name

NECA

Measurement

27nM - IC50

PubChem ID

3086599

Name

Cgs 21680

Measurement

2400nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Adenosine A3 receptor agonism may activate neutrophils, eosinophils and macrophages to produce cytokines useful in the treatment of inflammation, brain/cardiac ischemia and cancer, but may enhance mediator release from basophils and mast cells to augment asthma and other allergic conditions.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault