CA200689 CellAura fluorescent β2 antagonist [(S)-propranolol-red]

(HB7817)

Product overview

  • Name
    CA200689 CellAura fluorescent β2 antagonist [(S)-propranolol-red]
  • Short description
    Competitive fluorescent β2-adrenoceptor antagonist
  • Biological description
    Competitive fluorescent β2-adrenoceptor antagonist. Displays selectivity for β2 over β1 and β3 (apparent KD values are 9.21, 7.76 and 7.09 respectively). Antagonizes the activity of isoprenaline, a non-selective β-adrenoceptor agonist. Exhibits no intrinsic agonist activity.
  • Alternative names
    CA200689|;β2-633-AN2
  • Biological action
    Antagonist
  • Purity
    >97%
  • Citations

Images

Properties

  • Molecular Weight
    894
  • Source
    Synthetic
  • Formulation
    Lyophilized film
  • Excitation
    633 nm
  • Emission
    650 nm

Applications

  • Application notes
    For imaging at β1 / β2 / β3 adrenoceptors use solutions up to 100 nM.
  • Pharmacological validation
    The CellAura fluorescent β2 antagonist [(S)-propranolol-red] ligand was shown to antagonize the activity of the non-selective β agonist, isoprenaline, in three separate recombinant CHO cell lines expressing either the human β1, β2 or β3 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 β2 antagonist [(S)-propranolol-red] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent β2 antagonist [(S)-propranolol-red] has no intrinsic agonist activity at either β1, β2 or β3 receptors. To determine the apparent KD for CellAura fluorescent β2 antagonist [(S)-propranolol-red] at β1, β2 and β3 receptors, cells were treated with varying concentrations of isoprenaline alone, or in the presence of 1µM CellAura fluorescent β2 antagonist [(S)-propranolol-red], and the cyclic AMP-induced expression of SPAP measured. The apparent KD was calculated from the rightward shift of the agonist response curve in the presence of CellAura fluorescent β2 antagonist [(S)-propranolol-red], compared to the response curve for the agonist alone, for β1, β2 and β3 receptor expressing cell lines.

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 CA200689 CellAura fluorescent β2 antagonist [(S)-propranolol-red] (HB7817) 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!
  • Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.

    Baker JG et al. (2011) J Med Chem 54(19) : 6874-87.
    PubMedID: 21870877