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NK2 receptor ligand binding assay

The neurokinin (NK) 2 receptor is a member of the tachykinin family of G-protein-coupled receptors which also includes NK1 and NK3 receptors. The NK2 receptor is predominantly expressed in the periphery (inflammatory cells and bronchial, gastrointestinal and urinary smooth muscle) with limited expression in the CNS.

Tachykinin NK2 binding assay starter pack

Products Product reference Product insert MSDS
NK2 receptor red agonist - 5000 tests L0009RED pdf pdf
Tag-lite Tachykinin NK2 - 1 Million labeled cells C1TT1NK2 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 agonist is a Neurokinin A derivative labeled with a red emitting HTRF fluorescent probe
  • This ligand has been successfully used in a NK2 receptor Tag-lite binding assay.
  • Quantity/vial: 0.2nmol (dried)
  • Reconstitution Buffer: DMSO
  • Molecular Weight: 2001.4
Related products Product reference Product insert
Plasmid pSNAP-NK2 Tachykinin PSNAPNK2 pdf
Tag-lite SNAP-Lumi4Tb - 2 nmoles SSNPTBC -

Assay Validation:

 

NK2 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 L0009RED (Tag-lite NK2 receptor red agonist) 2 nM. Results obtained with radioligand assay and Tag-lite platform were very similar.

Family Receptor Compounds Radioactivity( Ki nM) Tag-lite (Ki nM)
Tachykinin NK2 Neurokinin A (agonist 2.0 (1) 5.7
GR159897 (antagonist) 0.32 (2) 1.1

(1) Appell et al. J. Biomol Screening, 1998
(2) Beresford et al. Eur J Pharmacol, 1995



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