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V2 receptor ligand binding assay

Vasopressin receptors are a group of G-protein-coupled receptors that mediate vasoconstriction, antidiuresis and ACTH release. They are currently divided into three subtypes, V1A, V1B and V2, and are closely related to oxytocin receptors (OT).

Vasopressin/Oxytocin V2 binding assay starter pack

Products Product reference Product insert MSDS
Vasopressin receptors red antagonist # 2- 5,000 tests L0001RED pdf pdf
Tag-lite Vassopressin V2 - 1 Million labeled cells C1TT1V2 Contact us -
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 europium 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 an Arginine-Vasopressin (AVP) derivative labelled with a Red Emitting HTRF fluorescent probe.
  • This ligand has been successfully used both in V2 receptor and V1A receptor Tag-lite binding assays.
  • Concentration: 10µM, HEPES pH 7.4 + 10% DMSO
  • Molecular Weight: 1760.7
Related products Product reference Product insert
Plasmid pSNAP-V2 PSNAPV2 pdf
Tag-lite SNAP-Lumi4Tb - 2 nmoles SSNPTBC -

Assay validation

 

Vasopressin V2 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 L0001RED (Tag-lite vasopressin receptors red antagonist #2) 10 nM.

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

Family Receptor Compounds Radioactivity( Ki nM) Tag-lite (Ki nM)
Vasopressin V2 AVP (agonist) 1.1(1) 0.9

(1) Durroux et al J Med Chem 1999



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