CA200645 CellAura fluorescent adenosine A3 antagonist [XAC]

(HB7812)
Technical documents: SDS CoA Datasheet

Product overview

Name CA200645 CellAura fluorescent adenosine A3 antagonist [XAC]
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
Purity >97%
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CA200645 CellAura fluorescent adenosine A3 antagonist [XAC]: Scientist Approved

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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Chemical Data

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:
  • Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation

    Cooper et al (2022) FASEB J. 36(4) : e2214
    PubMedID: 35230706
  • NanoBiT Complementation to Monitor Agonist-Induced Adenosine A<sub>1</sub> Receptor Internalization

    Soave M et al (2020) SLAS Discov 25(2) : 186-194
    PubMedID: 31583945
  • Probe dependence of allosteric enhancers on the binding affinity of adenosine A1 -receptor agonists at rat and human A1 -receptors measured using NanoBRET.

    Cooper SL et al (2019) Br J Pharmacol. : doi: 10.1111/bph.14575. [Epub ah
    PubMedID: 30644086
  • A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor.

    Bouzo-Lorenzo et al (2019) Purinergic Signal : doi: 10.1007/s11302-019-09650-9.
    PubMedID: 30919204
  • A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor.

    Bouzo-Lorenzo et al (2019) Purinergic Signal : doi: 10.1007/s11302-019-09650-9.
    PubMedID: 30919204

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