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Human AMY1R 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

Product Description and Product Data

This is an all-inclusive cell-based luciferase reporter assay kit targeting the the Human Amylin Type 1 Receptor (AMY1R). INDIGO’s AMY1R reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the AMY1R. In addition to AMY1R 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 AMY1R. 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 Mode
Kit Components
  • AMY1R Reporter Cells
  • Cell Recovery Medium (CRM)
  • Compound Screening Medium (CSM)
  • Human α-CGRP (100 μM in PBS+0.1%BSA)
  • Detection Substrate
  • Detection Buffer
  • 96-well, collagen-coated assay plate (white, sterile, cell-culture ready)
Shelf Life6 months
Shipping RequirementsDry Ice
Storage temperature-80C

Data

Activation of AMY1R. Assay was performed using the reference compound Human α-CGRP (Cayman Chemical, Ann Arbor, MI). Luminescence was quantified and values of average (n=3) relative light units (RLU), corresponding standard deviation (SD), Fold-Activation, and Z’ values were calculated. GraphPad Prism software was used to plot data using the least-squares method of non-linear regression for Fold-Activation vs. Log10 [α-CGRP, nM], and to determine the EC50 value.

Target Background

This assay utilizes proprietary human cells that provide constitutive expression of the receptors that comprise the Amylin Receptor Type 1 (AMY1R).

The Amylin receptors (AMY1-3R) are Class B G-protein coupled receptors formed by the heterodimerization of the calcitonin receptor (CTR) and one of the three Receptor Activity Modifying Proteins (RAMP1-3). These receptors have been identified as important drug targets due to their critical involvement in both metabolic control (e.g., energy balance and glucose homeostasis) and cognitive/neuroprotective effects.

The Amylin Receptor Type 1 (AMY1R) is one of three key receptors activated by the hormone amylin, also known as Islet Amyloid Polypeptide (IAPP), and is crucial for metabolic and cognitive health. Activation of AMY1R helps control key metabolic processes like gastric emptying, food intake, and postprandial glucose levels. Furthermore, the Calcitonin-Gene Related Peptide (CGRP), a neurotransmitter crucial in migraine pain, can bind and activate AMY1R, making the receptor a potential therapeutic target for migraine attacks. The binding of CGRP or Amylin to AMY1R stimulates G-Protein Gαs which activates adenylate cyclase (AC), leading to an increase in cellular cAMP. Due to the important physiological roles of AMY1R, the dysregulation of the receptor can lead to multiple diseases such as diabetes, obesity, and migraine. Importantly, the development of Dual Amylin and Calcitonin Receptor Agonists (DACRAs) is currently at the forefront of pharmaceutical strategies aimed at providing more effective and sustainable metabolic control for patients struggling with obesity and Type 2 Diabetes.

Citations

Also available as a service

Amylin Type 1 Receptor (AMY1R)

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