- Image Analysis:
Catalogue number: CA200689
Product: β2 antagonist [(S)-propranolol-red]
Selectivity: β1: 7.76 | β2: 9.21 | β3: 7.09
Labelled with BODIPY 630/650 (red)
|Pharmacophore||(S)-Propranolol-derivative||Catalogue Number||Pack Size||Price|
|Molecular Weight||894||CA200689-TK0*||0.05 mg||£137.50*|
|Excitation||633 nm||CA200689-050||0.5 mg||£1200|
|Emission||650 nm||CA200689-100||1.0 mg||£2150|
For imaging at β1 / β2 / β3 adrenoceptors use solutions up to 100 nM.
The CA200689 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 CA200689 to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CA200689 has no intrinsic agonist activity at either β1, β2 or β3 receptors.
To determine the apparent KD for CA200689 at β1, β2 and β3 receptors, cells were treated with varying concentrations of isoprenaline alone, or in the presence of 1µM CA200689, 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 CA200689, compared to the response curve for the agonist alone, for β1, β2 and β3 receptor expressing cell lines.