CA200634 CellAura fluorescent adenosine antagonist [XAC]

(HB7814)

Product overview

  • Name
    CA200634 CellAura fluorescent adenosine antagonist [XAC]
  • Short description
    Competitive fluorescent adenosine receptor antagonist
  • Biological description
    Competitive fluorescent adenosine receptor antagonist (apparent KD values are 7.50, 7.37 and 7.30 for A2A, A3 and A1 respectively). Antagonizes the activity of NECA, an adenosine receptor agonist. Inhibits cAMP accumulation and stimulates inositol phosphate accumulation (pKb values are 6.4 and 6.5 respectively). Exhibits no intrinsic agonist activity.
  • Alternative names
    Fluorescent Adenosine receptor Antagonist (A-633-AN), A-633-AN, XAC-X-BY630
  • Biological action
    Antagonist
  • Purity
    >97%
  • Our products in action

Images

Properties

  • Molecular Weight
    974
  • Source
    Synthetic
  • Appearance
    Purple solid
  • Formulation
    Lyophilized film
  • Excitation
    636 nm
  • Emission
    651 nm

Applications

  • Application notes
    For ligand binding; fluorescence imaging; high content analysis; kinetic analysis; cell sorting at adenosine A1 / A2A / A3 receptors use solutions up to 100 nM.
  • Pharmacological validation
    The CellAura fluorescent adenosine antagonist [XAC] ligand was shown to antagonize the activity of the adenosine receptor agonist adenosine-5'-N-ethyluronamide (NECA), in three separate recombinant CHO cell lines expressing the human A1, A2A or A3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.The cyclic AMP-induced expression of SPAP was measured under basal and forskolin-stimulated (maximal) conditions. Addition of CellAura fluorescent adenosine antagonist [XAC] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent adenosine antagonist [XAC] has no intrinsic agonist activity.To determine the apparent KD for CellAura fluorescent adenosine antagonist [XAC], cells were treated with varying concentrations of NECA alone, or in the presence of 1µM CellAura fluorescent adenosine antagonist [XAC], and the cyclic AMP-induced expression of SPAP measured.The apparent KD at A1, A2A and A3 receptors was calculated from the rightward shift of the agonist response curve in the presence of CellAura fluorescent adenosine antagonist [XAC], compared to the response curve for the agonist alone, for each receptor-expressing cell line.

Storing and Using Your Product

  • Storage instructions
    -20°C, protect from light
  • Solubility overview
    Soluble in DMSO
  • Handling
    After thawing individual aliquots for use, we recommend briefly sonicating the sample to ensure it is fully dissolved and the solution is homogeneous. We do not recommend using the product after subjecting it to repetitive freeze-thaw cycles.
  • Shipping conditions
    The product, supplied in a dry form, is stable at ambient temperature for periods of up to a few days and does not require shipping on ice/dry ice.
The following papers have cited the use of CA200634 CellAura fluorescent adenosine antagonist [XAC] (HB7814) from Hello Bio. If you have published a paper using this product, and it is not shown here, then please tell us! We will send you a free gift as a thank you!
  • Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers.

    Vernall AJ et al. (2013) Org Biomol Chem 11(34) : 5673-82.
    PubMedID: 23881285
  • Fluorescent ligands for adenosine receptors.

    Kozma E et al. (2013) Bioorg Med Chem Lett 23(1) : 26-36.
    PubMedID: 23200243
  • Antagonist selective modulation of adenosine A1 and A3 receptor pharmacology by the food dye Brilliant Black BN: evidence for allosteric interactions.

    May LT et al. (2010) Mol Pharmacol 77(4) : 678-86.
    PubMedID: 20086038
  • Pharmacology under the microscope: the use of fluorescence correlation spectroscopy to determine the properties of ligand-receptor complexes.

    Briddon SJ et al. (2007) Trends Pharmacol Sci 28(12) : 637-45.
    PubMedID: 18001848
  • Quantitative analysis of the formation and diffusion of A1-adenosine receptor-antagonist complexes in single living cells.

    Briddon SJ et al. (2004) Proc Natl Acad Sci U S A 101(13) : 4673-8.
    PubMedID: 15070776
  • Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor.

    Lane JR et al. (2010) Biochem Pharmacol 80(8) : 1180-9.
    PubMedID: 20599769
  • Fluorophore-tagged GPCR ligands.

    Middleton RJ et al. (2005) Curr Opin Chem Biol 9(5) : 517-25.
    PubMedID: 16125436
  • Selectivity of fluorescent ligands containing peptide-based linkers for the adenosine-A1 and -A3 receptors

    Stoddart LA et al. () Proceedings of the British Pharmacological Society :
  • Using the fluorescent antagonist, XAC-X-BY630 to quantify antagonist-adenosine A3 receptor complexes in membrane microdomains of single living cells.

    Corriden R et al. () Proceedings of the British Pharmacological Society :