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Human OXTR Reporter Assay Kit

SIZE SKU PRICE
1 x-96 well format assays
1 x-384 well format assays
SIZE SKU
1 x-384 well format assays
1 x-96 well format assays

Product Description and Product Data

This is an all-inclusive cell-based luciferase reporter assay kit targeting the Human Oxytocin Receptor (OXTR). INDIGO’s OXTR reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the OXTR. In addition to OXTR Reporter Cells, this kit provides two optimized media for use during cell culture and in diluting the user’s test samples, a reference agonist, Luciferase Detection Reagent, and a cell culture-ready assay plate. The principal application of this assay is in the screening of test samples to quantify any functional activity, either agonist or antagonist, that they may exert against OXTR. This kit provides researchers with clear, reproducible results, exceptional cell viability post-thaw, and consistent results lot to lot. Kits must be stored at -80C. Do not store in liquid nitrogen. Note: reporter cells cannot be refrozen or maintained in extended culture.

Features

  • Clear, Reproducible Results

  • All-Inclusive Assay Systems
  • Exceptional Cell Viability Post-Thaw
  • Consistent Results Lot to Lot

Product Specifications

Target TypeGPCR
SpeciesHuman
Receptor FormHybrid
Assay ModeAgonist, Antagonist
Kit Components
  • Human OXTR Reporter Cells
  • Cell Recovery Medium (CRM)
  • Compound Screening Medium (CSM)
  • Oxytocin, (ref. agonist; in PBS+0.1%BSA)
  • Detection Substrate
  • Detection Buffer
  • White, sterile, cell-culture ready assay plate
Shelf Life6 months
Shipping RequirementsDry Ice
Storage temperature-80C

Data

Activation of OXTR. Activation assays were performed using the reference compounds oxytocin (provided), the polypeptide Carbetocin, and the small-molecule drugs WAY 267464 and TC OT39. Luminescence was quantified and values of average (n = 3) relative light units (RLU), corresponding standard deviation (SD), Fold-Activation, and Z’ values were calculated. The least-squares method of non-linear regression was used to plot Fold-Activation or RLU vs. Log10 [Compound, nM] and EC50 / IC50 values were determined using GraphPad Prism software.
Inhibition of OXTR. OXTR reporter cells were co-treated with an EC80 concentration of the activator oxytocin and varying concentrations of the OXTR inhibitors, L-371,257, L-368,899, Atosiban, and PF-3274167. INDIGO’s Live Cell Multiplex (LCM) Assay confirmed that no treatment concentrations were cytotoxic (data not shown). Luminescence was quantified and values of average (n = 3) relative light units (RLU), corresponding standard deviation (SD), Fold-Activation, and Z’ values were calculated. The least-squares method of non-linear regression was used to plot Fold-Activation or RLU vs. Log10 [Compound, nM] and EC50 / IC50 values were determined using GraphPad Prism software.

Target Background

The oxytocin receptor (OXTR) is a member of the family of G-Protein-coupled receptors (GPCR). Its expression is distributed among many tissues, and it plays a wide variety of physiological roles both centrally and peripherally. For example, OXTR is highly expressed in peripheral tissues such as the uterus and the mammary glands to regulate the onset of labor1 and lactation. OXTR is also widely expressed in the neurons of the brain to regulate social behavior and cognition5. Several clinical trials indicate that exogenous administration of oxytocin may provide therapeutic benefit to alleviate psychiatric disorders including autism, schizophrenia, and mood disorders.

Oxytocin, the physiological activator of OXTR, is a nine amino acid neuropeptide that is synthesized in the hypothalamus and secreted from the posterior pituitary gland. Besides the use of oxytocin to induce labor, this peptide hormone has been clinically studied for the treatment of psychiatric disorders. Although the action of oxytocin rapidly elicits physiological effects in peripheral tissues, there are some challenges that limit its use as a treatment for psychiatric disorders. These include poor blood-brain barrier permeability, the size of the oligopeptide, and its relatively short half-life in vivo. To circumvent those issues the development of small molecules drugs with high affinities for OXTR and longer half-lives relative to oxytocin continue to be pursued. Indeed, non-peptide OXTR small molecule agonists and antagonists have been developed, and their efficacy as regulators of OXTR activity is demonstrated with this assay.

Also available as a service

Oxytocin Receptor (OXTR)

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