CA200645 CellAura fluorescent adenosine A3 antagonist [XAC]

(HB7812)
Technical documents: SDS CoA Datasheet

Product overview

Name CA200645 CellAura fluorescent adenosine A3 antagonist [XAC]
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
Purity >95%
Description Fluorescent A3 adenosine receptor antagonist
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Images

Figure 1. A3-SPAP cells assayed against NECA and 1 µM HB7812
Figure 2. A2A-SPAP cells assayed against NECA and 1 µM HB7812
Figure 3. A1-SPAP cells assayed against NECA and 1 µM HB7812

Fluorescence imaging with HB7812

HB7812 (100 nM) binding to live CHO cells expressing adenosine A3 receptors. (10 µM). Binding blocked by unlabelled competitor XAC. Nuclei counter-stained with Hoechst.
CA200645 CellAura fluorescent adenosine A3 antagonist [XAC]: Scientist Approved
CellAura fluorescent adenosine A3 antagonist [XAC] product vial image | Hello Bio

Biological Data

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

Solubility & Handling

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.

Calculators

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Dilution

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Chemical Data

Purity >95%
Molecular Weight 1144
Source Synthetic
Appearance Purple solid
Formulation Lyophilized film
Excitation 633 nm
Emission 650 nm
Publications
These publications cite the use of CA200645 CellAura fluorescent adenosine A3 antagonist [XAC] purchased from Hello Bio:
  • Involvement of β‐adrenoceptors in the cardiovascular responses induced by selective adenosine A2A and A2B receptor agonists

    Cooper et al (2022) Biorxiv : https://doi.org/10.1002/prp2.975
  • Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation

    Cooper et al (2022) FASEB J. 36(4) : e2214
    PubMedID: 35230706
  • Structure-based identification of dual ligands at the A2AR and PDE10A with anti-proliferative effects in lung cancer cell-lines

    Kalash L et al (2021) J Cheminform 13(1) : 17
    PubMedID: 33658076
  • Pharmacological characterisation of novel adenosine A3 receptor antagonists

    Barkan K et al (2020) Sci Rep 10(1) : 20781
    PubMedID: 33247159
  • Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells

    Stoddart LA et al (2020) Commun Biol 3(1) : 722
    PubMedID: 33247190

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