Fluorescent adrenoceptor β2 antagonist (apparent KD values are 8.87, 7.25 and 6.98 for β2, β1 and β3 respectively). Antagonizes the activity of isoprenaline, a non-selective β-adrenoceptor agonist.
For imaging at β1 / β2 / β3 adrenoceptors use solutions up to 100 nM.
Pharmacological validation
The CellAura fluorescent β2 antagonist [(±)-propranolol] 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. To determine the apparent KD for CellAura fluorescent β2 antagonist [(±)-propranolol] 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 [(±)-propranolol], 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 [(±)-propranolol], compared to the response curve for the agonist alone, for β1, β2 and β3 receptor expressing cell lines. The ACS β2 adrenoceptor CHO-K1 cell line was also transfected with the cAMP-responsive SPAP reporter construct and tested for its functional response to varying concentrations of isoprenaline alone, or in the presence of 1µM CellAura fluorescent β2 antagonist [(±)-propranolol].
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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CellAura Fluorescent Ligands technical FAQs (274.2 KB) ![CA200693 CellAura fluorescent β<sub>2</sub> antagonist [(S)-propranolol-green]](https://hellobio.com/media/catalog/product/cache/5e99c5642d3d759e334623db25363a04/h/b/hb7816-ca200693-image1_1.png)
