Adenosine A1 receptor expressing cells labeled with Terbium

Tag-lite cells transiently expressing the A1 receptor labeled with Terbium for use in receptor binding applications. The cells are provided ready to use.

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  • Fully functional cell line
  • Transient expression
  • Cellular binding assay

Tag-lite cells transiently expressing the A1 receptor labeled with Terbium for use in receptor binding applications. The cells are provided ready to use.

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Overview

A1 receptor is one of the four adenosine receptor family (including A2A, A2B and A3 receptors).  It has vital role in cardiac and renal processes. It regulates neurotransmitters in the brain, such as dopamine and glutamate. Thus, it is considered as an interesting target in treatment of ischemia-reperfusion injury, renal pathologies, and neuropathic pain.

Cells expressing the A1 receptor are provided pre-labeled with Terbium, and can be used to conduct receptor binding studies on the aforementioned receptor.

Benefits

  • PRE-LABELED WITH TERBIUM
  • FROZEN CELLS, READY TO BE USED
  • CELLS/LIGAND VALIDATED FOR BINDING

Assay principle

Running your A1 receptor binding assay using Tag-lite is as easy as it can get. Simply dispense 10 µL of labeled cells (C1TT1A1) into each well, followed by 5 µL of labeled ligand (L0067RED) 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.

Watch this videoexplaining how to run a saturation binding assay using Tag-lite.

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.
Watch this video explaining how to run a competitive binding assay using Tag-lite.

Kd and Ki validation

Examples of data obtained using Adenosine A1 receptor labeled cells and their matching fluorescent ligand (L0067RED). XAC (Xanthine amine congener) was used for Ki determination in the competitive binding assay. Results may vary from one HTRF® compatible reader to another.

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