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GABA-B receptor ligand binding assay

GABA-B binding assay starter pack

Products Product reference Product insert MSDS
Tag-lite GABAB receptor red antagonist - 5,000 tests L0014RED pdf pdf
Tag-lite GABA-B - 1 Million labeled cells C1TT1GABAB 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 antagonist is a CGP-54626 derivative labeled with a red emitting HTRF fluorescent probe
  • This ligand has been successfully used in a GABAB receptor Tag-lite binding assay
  • Developed under collaboration with CellAura
  • Concentration: 10µM
  • Volume: 250µL
  • Buffer: HEPES 50mM, pH7.4 + 10% DMSO
  • Molecular Weight: 1044
Related products Product reference Product insert
Plasmid pSNAP-GABA-B PSNAPGABAB pdf
Tag-lite SNAP-Lumi4Tb - 2 nmoles SSNPTBC -

Assay Validation:

 

GABA-B 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 L0014RED (Tag-lite GABAB receptors red antagonist) 25 nM.

Results obtained with radioligand assay and Tag-lite platform were very similar.

Family Receptor Compounds Radioactivity
(Ki nM)
Tag-lite
(Ki nM)
GABA GABA-B CGP-5426 8.13 (1) 3.9

(1) Woods et al Br J Pharmacol, 2000



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