CGP 20712 dihydrochloride

Cat. No. 1024

CGP 20712 dihydrochloride C23H25F3N4O5.2HCl [1216905-73-5]

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Chemical Name: 1-[2-((3-Carbamoyl-4-hydroxy)phenoxy)ethylamino]-3-[4-(1-methyl-4-trifluoromethyl-2-imidazolyl)phenoxy]-2-propanol dihydrochloride

Biological Activity

Highly selective and potent β1-adrenoceptor antagonist (IC50 = 0.7 nM). Displays 10,000-fold selectivity over β2-adrenoceptors. Also available as part of the β-Adrenoceptor Antagonist Tocriset™.

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Hieble et al (1995) α-and β-adrenoceptors. From the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J.Med.Chem. 38 3415. PMID: 7658428.

Kitagawa et al (1995) Determination of β-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective β-antagonists. Br.J.Pharmacol. 116 1635. PMID: 8564230.

Dooley et al (1986) CGP 20712A: a useful tool for quantitating β1- and β2-adrenoceptors. Eur.J.Pharmacol. 130 137. PMID: 2877892.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for CGP 20712 dihydrochloride include:

Creed et al (2015) β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion. Breast Cancer Res 17 145. PMID: 26607426.

Littmann et al (2015) Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands. J Biol Chem 355 183. PMID: 26306764.

Weiterer et al (2015) Galactomannan and Zymosan Block the Epinephrine-Induced Particle Transport in Tracheal Epithelium. J Neurochem 10 e0143163. PMID: 26571499.

Gherbi et al (2014) Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP. Br J Pharmacol 171 5431. PMID: 25052258.

Lavine et al (2013) Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism. JAMA Ophthalmol 131 376. PMID: 23303344.

Mistry et al (2013) Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists. J Med Chem 56 3852. PMID: 23614528.

Cheng et al (2012) Cytoskeletal role in protection of the failing heart by β-adrenergic blockade. Am J Physiol Heart Circ Physiol 302 H675. PMID: 22081703.

Hott et al (2012) Both α1- and β1-adrenoceptors in the bed nucleus of the stria terminalis are involved in the expression of conditioned contextual fear. Br J Pharmacol 167 207. PMID: 22506532.

Rieg et al (2012) Cardiovascular agents affect the tone of pulmonary arteries and veins in precision-cut lung slices. PLoS One 6 e29698. PMID: 22216346.

Rankovic et al (2011) Modulation of calcium-dependent inactivation of L-type Ca2+ channels via β-adrenergic signaling in thalamocortical relay neurons. PLoS One 6 e27474. PMID: 22164209.

Sucharov et al (2011) β-Adrenergic receptor stimulation and activation of protein kinase A protect against α1-adrenergic-mediated phosphorylation of protein kinase D and histone deacetylase 5. Circulation 17 592. PMID: 21703532.

Crestani et al (2008) Both alpha1 and alpha2-adrenoceptors mediate the cardiovascular responses to noradrenaline microinjected into the bed nucleus of the stria terminal of rats. Br J Pharmacol 153 583. PMID: 18037912.

Lemke et al (2008) Unchanged β-adrenergic stimulation of cardiac L-type calcium channels in Ca v 1.2 phosphorylation site S1928A mutant mice. PLoS One 283 34738. PMID: 18829456.

Jane-Wit et al (2007) β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis. J Pharmacol Exp Ther 116 399. PMID: 17620508.

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