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.
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.
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.
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.
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