CA200656 CellAura fluorescent β2 antagonist [(±)-propranolol]

(HB7820)
Technical documents: SDS CoA Datasheet

Product overview

Name CA200656 CellAura fluorescent β2 antagonist [(±)-propranolol]
Biological description 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.
Alternative names CA200656|β2-633-AN
Purity >97%
Description Fluorescent β2 adrenoceptor antagonist
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Images

Figure 1. β1-SPAP cells assayed against lsoprenaline and 1 µM HB7820

Fluorescence imaging with HB7820

Figure 2. β2-SPAP cells assayed against Isoprenaline and 1µM HB7820

Fluorescence imaging with HB7820

HB79820 ligand binding and displacement. (A, C, E): HB7820 ligand (A: 20 nM, C, E: 100 nM) binding to three different live cell lines expressing β2-adrenoceptors. (B,D,F): binding blocked by unlabelled competitor ICI118551 (10 µM). Nuclei counter-stained with Hoechst.
Fluorescence imaging with HB7820
CA200656 CellAura fluorescent β2 antagonist [(±)-propranolol]: Scientist Approved
CellAura fluorescent β2 antagonist [(±)-propranolol] product vial image | Hello Bio

Biological Data

Application notes 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.

Calculators

Molarity

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Dilution

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Chemical Data

Purity >97%
Molecular Weight 834
Formulation Lyophilized film
Excitation 633 nm
Emission 650 nm
Publications
These publications cite the use of CA200656 CellAura fluorescent β2 antagonist [(±)-propranolol] purchased from Hello Bio:
  • Measuring ligand binding kinetics to membrane proteins using virion nano-oscillators.

    Ma et al (2018) J Am Chem Soc doi: 10.1021 : /jacs.8b07461.
    PubMedID: 30114365
  • 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

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