CGP 20712 dihydrochloride
1 Image
Description: Highly potent and selective β1 antagonist
Chemical Name: 1-[2-((3-Carbamoyl-4-hydroxy)phenoxy)ethylamino]-3-[4-(1-methyl-4-trifluoromethyl-2-imidazolyl)phenoxy]-2-propanol dihydrochloride
Purity: ≥96%
Biological Activity
CGP 20712 dihydrochloride is a highly selective and potent β1-adrenoceptor antagonist (IC50 = 0.7 nM). Displays 10,000-fold selectivity over β2-adrenoceptors.Technical Data
M.Wt:
567.39
Formula:
C23H25F3N4O5.2HCl
Solubility:
Soluble to 50 mM in water
Purity:
≥96%
Storage:
Desiccate at +4°C
CAS No:
1216905-73-5
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Protein kinase A activation inhibits DUX4 gene expression in myotubes from patients with facioscapulohumeral muscular dystrophy
JM Cruz, N Hupper, LS Wilson, JB Concannon, Y Wang, B Oberhauser, K Patora-Kom, Y Zhang, DJ Glass, AU Trendelenb, BA Clarke
J. Biol. Chem., 2018;0(0):. -
Role of AKAP79/150 protein in beta1-adrenergic receptor trafficking and signaling in mammalian cells.
Li X, Nooh M, Bahouth S
J Biol Chem, 2013;288(47):33797-812. -
CGP 20712A: a useful tool for quantitating β1- and β2-adrenoceptors.
Dooley et al.
Eur.J.Pharmacol., 1986;130:137 -
α and β-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Heible et al.
J.Med.Chem., 1995;38:3415 -
Determination of β-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective β-antagonists.
Kitagawa et al.
Br.J.Pharmacol., 1995;116:1635 -
α-and β-adrenoceptors. From the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Hieble et al.
J.Med.Chem., 1995;38:3415
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Citations for CGP 20712 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for CGP 20712 dihydrochloride include:
16 Citations: Showing 1 - 10
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β2-Adrenergic Receptor Antagonism Attenuates CNV Through Inhibition of VEGF and IL-6 Expression.
Authors: Lavine
Invest Ophthalmol Vis Sci 2017;58(1):299
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Modulation of neuroinflammation and pathology in the 5XFAD mouse model of Alzheimer's disease using a biased and selective beta-1 adrenergic receptor partial agonist.
Authors: Ardestani Et al.
Neuropharmacology 2017;116:371
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Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.
Authors: Littmann Et al.
J Biol Chem 2015;355:183
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β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion.
Authors: Creed Et al.
Breast Cancer Res 2015;17:145
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Galactomannan and Zymosan Block the Epinephrine-Induced Particle Transport in Tracheal Epithelium.
Authors: Weiterer Et al.
J Neurochem 2015;10:e0143163
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Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP.
Authors: Gherbi Et al.
Br J Pharmacol 2014;171:5431
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Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
Authors: Mistry Et al.
J Med Chem 2013;56:3852
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Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism.
Authors: Lavine Et al.
JAMA Ophthalmol 2013;131:376
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Cardiovascular agents affect the tone of pulmonary arteries and veins in precision-cut lung slices.
Authors: Rieg Et al.
PLoS One 2012;6:e29698
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Cytoskeletal role in protection of the failing heart by β-adrenergic blockade.
Authors: Cheng Et al.
Am J Physiol Heart Circ Physiol 2012;302:H675
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Both α1- and β1-adrenoceptors in the bed nucleus of the stria terminalis are involved in the expression of conditioned contextual fear.
Authors: Hott Et al.
Br J Pharmacol 2012;167:207
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Modulation of calcium-dependent inactivation of L-type Ca2+ channels via β-adrenergic signaling in thalamocortical relay neurons.
Authors: Rankovic Et al.
PLoS One 2011;6:e27474
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β-Adrenergic receptor stimulation and activation of protein kinase A protect against α1-adrenergic-mediated phosphorylation of protein kinase D and histone deacetylase 5.
Authors: Sucharov Et al.
Circulation 2011;17:592
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Unchanged β-adrenergic stimulation of cardiac L-type calcium channels in Ca v 1.2 phosphorylation site S1928A mutant mice.
Authors: Lemke Et al.
PLoS One 2008;283:34738
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Both alpha1 and alpha2-adrenoceptors mediate the cardiovascular responses to noradrenaline microinjected into the bed nucleus of the stria terminal of rats.
Authors: Crestani Et al.
Br J Pharmacol 2008;153:583
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β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis.
Authors: Jane-Wit Et al.
J Pharmacol Exp Ther 2007;116:399
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