CA200645 CellAura fluorescent adenosine A3 antagonist [XAC]

(HB7812)

Product overview

  • Name
    CA200645 CellAura fluorescent adenosine A3 antagonist [XAC]
  • Short description
    Fluorescent A3 adenosine receptor antagonist
  • Biological description
    Fluorescent A3 adenosine receptor antagonist. Displays selectivity for A3 over A2A and A1 (apparent KD values are 8.10, 6.74 and 6.57 respectively). Antagonizes the activity of NECA, an adenosine receptor agonist. Exhibits no intrinsic agonist activity. A fluorescent Xanthine Amine Congener (XAC) analog.
  • Alternative names
    Fluorescent Adenosine A3 receptor Antagonist (A3-633-AN), A3-633-AN
  • Biological action
    Antagonist
  • Purity
    >97%
  • Our products in action

Images

Properties

  • Molecular Weight
    1144
  • Source
    Synthetic
  • Appearance
    Purple solid
  • Formulation
    Lyophilized film
  • Excitation
    633 nm
  • Emission
    650 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 A3 antagonist [XAC] ligand was shown to antagonize the activity of the adenosine receptor agonist, 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 A3 antagonist [XAC] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent adenosine A3 antagonist [XAC] has no intrinsic agonist activity. To determine the apparent KD for CellAura fluorescent adenosine A3 antagonist [XAC], cells were treated with varying concentrations of NECA alone, or in the presence of 1µM CellAura fluorescent adenosine A3 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 A3 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.
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
The following papers have cited the use of CA200645 CellAura fluorescent adenosine A3 antagonist [XAC] (HB7812) 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!
  • Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes.

    Corriden R et al. (2013) EMBO Rep 14(8) : 726-32.
    PubMedID: 23817552
  • 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
  • Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay.

    Stoddart LA et al. (2012) Chem Biol 19(9) : 1105-15.
    PubMedID: 22999879