Adenosine A2AR fluorescent probe
Tag-lite Adenosine A2A receptor fluorescent probe
One of four adenosine receptors found in the brain, A2A is a GPCR. A2A receptor is thought to play a role in acute and chronic neurodegenerative disorders such as cerebral ischemia or Parkinson's disease. A2A may also be involved in seizures and sleep disorders.
Cells expressing the A2A receptor are provided pre-labeled with Terbium, and can be used to conduct receptor binding studies on the aforementioned receptor.
Watch this video explaining how to run a saturation binding assay using Tag-lite.
Watch this video explaining how to run a competitive binding assay using Tag-lite.
Examples of data obtained using A2A labeled cells and their matching fluorescent ligand (L0058RED). ZM-241385 was used as reference ligand. Results may vary from one HTRF® compatible reader to another.
Adenosine receptors designated by four subtypes A1, A2A, A2B and A3 were shown to be promising pharmacological targets for the development of therapeutic compounds for various therapeutic areas such as cancer, neurodegenerative disease and COPD/Asthma. Thus, a wide range of compounds, and particularly antagonists have been largely studied.
The Tag-Lite® binding assay platform offers the complete adenosine receptors subset A1, A2A, A2B and A3 to characterize compounds in term of binding affinity (Ki) and selectivity profile.
The set of compounds have been profiled on A1, A2A, A2B and A3 receptors using their respective fluorescent ligands L0067RED, L0058RED, L0068RED and L0069GRE.The selectivity profiles of several compounds involved in different therapeutic areas were assessed with this Tag-Lite platform.
The table below summarizes the resulting Ki obtained for each receptor subtype for the full panel of compounds. The results are confirming the expected selectivity and the range of affinities for these reference compounds.
Compound | Pharmacological class | Compounds affinities (Ki - nM) for the different adenosine receptor subtypes | |||
A1 | A2A | A2B | A3 | ||
XAC | Non selective antagonist | 12 | 15 | 20 | 50 |
Theophylline | Non selective antagonist | 4000 | 5000 | 18000 | 140000 |
DPCPX | A1 antagonist | 7.6 | 170 | 145 | 800 |
Vipadenant | A2A antagonist | 70 | 0.9 | 55 | 20000 |
Ciforadenant (CPI-444) | A2A antagonist | 150 | 3.4 | 660 | 1600 |
Preladenant (SCH 420814) | A2A antagonist | > 20 000 | 5 | > 20 000 | >20 000 |
Istradefylline (KW-6002) | A2A antagonist | >10 000 | 40 | >10 000 | >10 000 |
ZM241385 | A2A antagonist | 260 | 0.7 | 40 | 750 |
AZD4635 | A2A antagonist | 900 | 15 | 660 | > 10 000 |
MRS1706 | A2B inverse agonist | 150 | 325 | 30 | > 300 |
MRS1220 | A3 antagonist | 325 | 37 | > 500 | 1.6 |
The graphs show the pattern of the dose-response curves obtained for five compounds displaying different selectivity profile.
In collaboration with Boehringer Ingelheim - Présentations scientifiaues
In collaboration with Bayer - Présentations scientifiaues
The easy way to approach biology without radioactivity - Flyers
Challenge the limits of binding kinetics studies - Notes d'application
Binding Assays to measure therapeutic antitumor antibodies - Posters
In collaboration with GEN - Guides
Featuring a panel of experts - Vidéos
The gold standard technology for receptor binding studies - Vidéos
C1TT1A2A Lot 14 - Protocoles
All your HTRF assays in one document! - Catalogue
General principles of HTRF - Guides
Case study about kinetic binding characterization provided by the combination of Cisbio and Excellerate bioscience expertise. - Notes d'application
Get the brochure about technology comparison. - Brochures
Available On-demand - Vidéos
How to revolutionize your kinetic binding demonstration with HTRF kinase binding platform assays - Notes d'application
C1TT1A2A - Fiches de sécurité
C1TT1A2A - Fiches de sécurité
C1TT1A2A - Fiches de sécurité
C1TT1A2A - Fiches de sécurité
C1TT1A2A - Fiches de sécurité
C1TT1A2A - Fiches de sécurité
C1TT1A2A - Fiches de sécurité