View the slide viewer

Have questions about this assay kit?

Human ADRA1A Reporter Assay Kit

1 x-384 well format assays
1 x-96 well format assays
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 the Human Adrenoreceptor Alpha 1A (ADRA1A). INDIGO’s ADRA1A reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the ADRA1A. In addition to ADRA1A 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 ADRA1A. 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.


  • Clear, Reproducible Results

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

Product Specifications

Target TypeGPCR
Receptor FormHybrid
Assay ModeAgonist, Antagonist
Kit Components
  • Human ADRA1A Reporter Cells
  • Cell Recovery Medium (CRM)
  • Compound Screening Medium (CSM)
  • L-Phenylephrine, (ref. agonist; in DMSO)
  • Detection Substrate
  • Detection Buffer
  • White, sterile, cell-culture ready assay plate
Shelf Life6 months
Shipping RequirementsDry Ice
Storage temperature-80C


Activation of ADRA1A. Activation assays were performed using the reference compounds L-phenylephrine, A-61603, Norepinephrine and Clonidine. The absence of signal in L-Phenylephrine treated ‘Mock’ cells (which contains the NFAT-Luc reporter vector, but do not express ADRA1A) confirms that the observed ligand-dependent response is specific to ADRA1A activation.
Inhibition of ADRA1A. ADRA1A reporter cells were co-treated with an EC80 concentration of the reference activator L-phenylephrine and varying concentrations of the ADRA1A specific inhibitors Niguldipine and Silodosin, and the general alpha adrenergic receptor inhibitors Tamsulosin, WB4101, Prazosin, and BMY7378. 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. Non-linear regression analyses of Fold-Activation or RLU vs. Log10 [Compound, nM] and EC50 / IC50 values were determined using GraphPad Prism software.

Target Background

The adrenoreceptors (a.k.a. adrenergic receptors) mediate the action of the sympathetic nervous system and are activated in response to “fight-or-flight” signals. They are divided into three types, adrenoreceptor α1-, α2-, and β. Each type is further composed of three subtypes resulting in 9 different types (α1A, α1B, α1D, α2A, α2B, α2C, β1, β2, and β3). Adrenoreceptors belong to the G-Protein-coupled receptor (GPCR) family. They all display the characteristic seven transmembrane helices, the extracellular loops which contribute to ligand binding, and the intracellular carboxy tail that associates with trimeric G proteins. All nine types of adrenoreceptors are activated by the same endogenous catecholamines (epinephrine and norepinephrine); however, the specificity of their responses depends on the G-proteins and effectors systems they associate with in a tissue and time specific manner.

Adrenoreceptor alpha1A (ADRA1A) signals through the Gαq/11 family of G proteins. Upon binding to a catecholamine, ADRA1A undergoes a conformational change that triggers the activation of Gaq/11 proteins via an exchange of GDP with GTP, followed by the activation of phospholipase C, the release of inositol triphosphate (IP3) which binds to its receptors on the endoplasmic reticulum and triggers the release of calcium and activation of the protein kinase C.

ADRA1A is expressed in cardiac myocytes, in vascular smooth muscles cells of blood vessels and urinary tract and in the brain. It plays an important role in the regulation of blood pressure, glucose metabolism, lipid metabolism, and leptin secretion. In addition, ARA1A has a neuroprotective role and is of interest in the development of therapeutics for the treatment of neurological conditions such as Alzheimer’s disease and dementia.

Also available as a service

Adrenoreceptor Alpha 1A (ADRA1A)

Have questions about this assay kit?