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Human GHSR1a Reporter Assay Kit

SIZE SKU PRICE
1 x-96 well format assays—
3 x-32 assays in-96 well format—
SIZE SKU
3 x-32 assays in-96 well format
1 x-96 well format assays
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Product Description and Product Data

This is an all-inclusive cell-based luciferase reporter assay kit targeting the the Human Growth Hormone Secretagogue Receptor Type 1a (GHSR1a). INDIGO’s GHSR1a reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the GHSR1a. In addition to GHSR1a 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 GHSR1a. 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 ModeInverse Agonist
Kit Components
  • GHSR1a Reporter Cells
  • Cell Recovery Medium (CRM)
  • Compound Screening Medium (CSM)
  • PF-05190457
  • Detection Substrate
  • Detection Buffer
  • White, sterile, cell-culture ready assay plate
Shelf Life6 months
Shipping RequirementsDry Ice
Storage temperature-80C

Data

The Human GHSR1a Inverse-Agonist Assay. Dose-response analyses of the GHSR1a Inverse-Agonist Assay were performed using the inverse-agonist PF-05190457 (provided as reference; Cayman Chemical, USA). GHSR1a Inverse-Agonist Assay setup was performed as described in this Technical Manual. Relative Light Units were quantified and average values of RLU and their respective values of relative standard deviation were determined for each treatment concentration. Non-linear regression analyses were performed and IC50 values determined using GraphPad Prism software. The high Z' value confirms the robust performance of this assay, and its suitability for HTS applications.

Target Background

GHSR1a, also known as Ghrelin Receptor, is a class A G protein-coupled receptor (GPCR) that plays a crucial role in regulating food intake, body weight, glucose homeostasis, and other essential physiological functions.

GHSR1a is activated by ghrelin, a peptide hormone primarily secreted by endocrine cells in the oxyntic mucosa of the stomach. GHSR1a can also adopt constitutively active conformational states, enabling ligand-independent signaling. Its high basal activity makes it particularly responsive to inverse agonists, such as liver-enriched antimicrobial peptide-2 (LEAP2), which serves as both an endogenous competitive antagonist of ghrelin and an inverse agonist that suppresses constitutive GHSR1a signaling. Upon activation, GHSR1a signals through the Gαq/11 pathway, activating phospholipase C (PLC), which leads to an increase in intracellular calcium levels. This is the signaling pathway utilized in this reporter assay.

Modulation of GHSR1a offers a dual therapeutic strategy. Inverse agonists and antagonists are being explored as anti-obesity agents, with the goal of promoting weight loss and improving insulin sensitivity. Conversely, GHSR1a agonists are investigated for their potential to stimulate neurogenesis and improve cognitive function in patients with cognitive decline. This bidirectional approach underscores the significance of GHSR1a as a drug target and has promoted considerable interest in innovative therapies addressing both metabolic and neurological disorders.

Citations

Also available as a service

GHSR1a, Growth Hormone Secretagogue Receptor Type 1a

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