Fluorescent β2-adrenoceptor antagonist (apparent KD values are 7.68, 6.42 and <4.0 for β2, β1 and β3 respectively). Antagonizes the activity of isoprenaline, a non-selective β-adrenoceptor agonist. Exhibits no intrinsic agonist activity.
Figure 1. β2-SPAP cells assayed against Isoprenaline and HB7816
Figure 2. β1-SPAP cells assayed against lsoprenaline and HB7816
Figure 3. β3-SPAP cells assayed against Isoprenaline and HB7816
Fluorescence imaging with HB7816
HB7816(30 nM) binding to live CHO cells expressing β2 adrenergic receptors. Binding blocked by unlabelled competitor ICI118551 (1 µM). Nuclei counter-stained with Draq5.
Figure 1. β2-SPAP cells assayed against Isoprenaline and HB7816
Figure 2. β1-SPAP cells assayed against lsoprenaline and HB7816
Figure 3. β3-SPAP cells assayed against Isoprenaline and HB7816
Fluorescence imaging with HB7816
HB7816(30 nM) binding to live CHO cells expressing β2 adrenergic receptors. Binding blocked by unlabelled competitor ICI118551 (1 µM). Nuclei counter-stained with Draq5.
For imaging at β1 / β2 / β3 adrenoceptors use solutions up to 100 nM.
Pharmacological validation
The CellAura fluorescent β2 antagonist [(S)-propranolol-green] 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-green] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent β2 antagonist [(S)-propranolol-green] has no intrinsic agonist activity at either β1, β2 or β3 receptors. To determine the apparent KD for CellAura fluorescent β2 antagonist [(S)-propranolol-green] 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-green], 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-green], compared to the response curve for the agonist alone, for β1, β2 and β3 receptor expressing cell lines.
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.
These publications cite the use of CA200693 CellAura fluorescent β2 antagonist [(S)-propranolol-green] purchased from Hello Bio:
Development of fluorescent peptide G protein-coupled receptor activation biosensors for NanoBRET characterization of intracellular allosteric modulators.
Farmer JP et al (2022) FASEB journal : official publication of the Federation of American Societies for Experimental Biology 36 : e22576
Development of fluorescent peptide G Protein Coupled Receptor activation biosensors for NanoBRET characterisation of intracellular allosteric modulators
Holliday et al (2022) Biorxiv : https://doi.org/10.1101/2022.05.30.494024
Charge-Sensitive Optical Detection of Small Molecule Binding Kinetics in Normal Ionic Strength Buffer
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CellAura Fluorescent Ligands technical FAQs (274.2 KB) ![CA200689 CellAura fluorescent β<sub>2</sub> antagonist [(S)-propranolol-red]](https://hellobio.com/media/catalog/product/cache/5e99c5642d3d759e334623db25363a04/h/b/hb7817-ca200689-image1_1.png)
