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HTRF Tag-Lite Adenosine A2b Receptor Cells, 200 Assay Points

Tag-lite cells transiently expressing the A2B receptor labeled with Terbium for use in receptor binding applications. The cells are provided ready to use.

For research use only. Not for use in diagnostic procedures.

Part number: C1TT1A2B
Unit Size: 200 Assay Points
List price: USD 1,030.00
Your price:
USD 1,030.00
USD 1,030.00 /each


A2B receptor is one of the four adenosine receptor family (including A1, A2A, and A3 receptors). A2B is involved in processes such as inflammation, immune responses, vasodilation, cell growth, intestinal function, and neurosecretion. Thus, it is considered as an interesting target in the treatment of cancer, diabetes, renal disease, and vascular disease.

Cells expressing the A2B receptor are provided pre-labeled with Terbium, and can be used to conduct receptor binding studies on the aforementioned receptor.


Assay Points
Assay Target Type
Assay Technology
Shelf Life
540.0 Day(s)
Shipping Conditions
Shipped in Dry Ice
Therapeutic Area
Infectious Diseases
Oncology & Inflammation
Rare Diseases
Unit Size
200 Assay Points

Video gallery

How it works

Assay principle

Running your A2B receptor binding assay using Tag-lite is as easy as it can get. Simply dispense 10 µL of labeled cells (C1T1A2B) into each well, followed by 5 µL of labeled ligand (L0068RED) and 5 µL of the compound you wish to test. Like all HTRF assays, Tag-lite assays do not require any washing steps. A diagram of the procedure to be followed is given on the right.

Saturation binding (KD)

A saturation binding assay measures total and non-specific binding for increasing concentrations of ligand under equilibrium conditions. To perform the assay, the fluorescent ligand is titrated into a solution containing a fixed amount of labeled cells, and then incubated to equilibrium. The HTRF Ratio obtained from this titration is the total binding.

Competitive binding (KI)

A competitive binding assay is performed to measure the dissociation constant, Ki. To perform the assay, the compound is titrated into a solution containing a fixed concentration of fluorescent ligand and a fixed amount of cells.



Assay validation

Kd and Ki validation

Examples of data obtained using Adenosine A2B receptor labeled cells and their matching fluorescent ligand (L0068RED). XAC (Xanthine amine congener) was used for Ki determination in the competitive binding assay. Results may vary from one HTRF® compatible reader to another.

Compound profiling on Adenosine A1, A2A, A2B and A3 receptors

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 14000
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 >20000 5 >20000 >20000
Istradefylline (KW-6002) A2A antagonist >10000 40 >10000 >10000
ZM241385 A2A antagonist 260 0.7 40 750
AZD4635 A2A antagonist 900 15 660 >10000
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.






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Tag-lite™ is a cell-based, no-wash alternative to traditional radioisotope assays for studying GPCR-ligand interaction.


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