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Beta2 receptor ligand binding assay

Adrenergic beta 2 binding assay starter pack

Products Product reference Product insert MSDS
Beta2 adrenergic receptor green antago - 5000 tests L0011GRE pdf pdf
Tag-lite Adrenergic beta2 - 1 Million labeled cells C1TT1BETA2 pdf -
Tag-lite buffer - 100 ml (5X) LABMED - -

The binding assay starter pack consists of three references, the labeled cells, the fluorescent ligand and the Tag-lite buffer. Each component must be ordered separately. The cells express the SNAP-receptor labeled with terbium cryptate (labeling performed with Tag-lite SNAP-Lumi4 Tb). The labeled cells are proposed in a 1 million cell pack, to achieve a minimum of 100 tests at a cell density of 10,000 cells/well.

Features:
  • This beta2 adrenoceptor antagonist is a propranolol derivative labeled with a green emitting HTRF fluorescent probe. This product was co-developed with CellAura Technologies to be used in conjunction with Cisbio's Tag-lite® technology platform.
  • This ligand has been successfully used in a beta2-adrenergic Tag-lite binding assay
  • Concentration: 10µM
  • Buffer: HEPES pH7.4 + 10% DMSO
  • Molecular Weight: 760
Related products Product reference Product insert
Plasmid pSNAP-Beta2 PSNAPBD2 pdf
Tag-lite SNAP-Lumi4Tb - 2 nmoles SSNPTBC -

Assay Validation:

 

Beta2 receptor ligand binding assay was performed using the starter pack reagents.

Kd was determined and signal inhibition (IC50) by agonist and antagonist was performed with L0011GRE (Tag-lite beta adrenergic receptor green antagonist) 6nM. Results obtained with radioligand assay and Tag-lite platform were very similar.

Family Receptor Compounds Radioactivity( Ki nM) Tag-lite (Ki nM)
Adrenergic beta2 Isoproterenol (1) - Agonist 387 425
Alprenolol (2) - Antagonist 1 0.40
ICI 118551 (2) - Antagonist 0.31 - 0.63 0.33

(1) Sato et al. Eur J Pharmacol, (1996) 315, 363-367
(2) Baker et al. Eur J Pharmacol, (2005) 144, 317-322



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