CA200693 CellAura fluorescent β2 antagonist [(S)-propranolol-green](HB7816)
CA200693 CellAura fluorescent β2 antagonist [(S)-propranolol-green]
Fluorescent β2-adrenoceptor antagonist
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.
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525 / 550nm
For imaging at β1 / β2 / β3 adrenoceptors use solutions up to 100 nM.
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.
Storing and Using Your Product
-20°C, protect from light
Soluble in DMSO
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.
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.
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
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
Reviews & Product Guides
In my experiments seems to have quite a high non-specific binding at working concentrations. To work with the (S)-PROPRANOLOL-GREEN for competition experiments you have to use 100-200nM concentration. Even if I have not finished the optimization of my experiments yet, the compound seems to show quite a lot of non-specific binding at these concentrations, thus limiting their use for pharmacological experiments. Maybe using HTRF, for which this compound is compatible, the problem could be solved. I will switch to a higher affinity ligand to decrease the concentration needed.
>>>Response from Hello Bio Technical Support:>>>
Many thanks for leaving us your feedback on the (S)-propranolol-green fluorescent ligand (HB7816). As you were finding some non-specific biding, I wanted to send you some documentation that may be of some help.
I have attached a ‘getting started guide’ which includes an example protocol for a typical fluorescent ligand binding and displacement assay and an example FACS application note (which uses a fluorescent D1 receptor antagonist). Finally, I have also attached some technical FAQs which may be of some help.
I hope this helps. If you have any questions please do not hesitate to contact me and if you require a free of charge replacement to try the compound again, please let me know and we will send one to you.
Hello Bio Technical Support