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Submit ReviewCGP 20712 dihydrochloride
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% (HPLC)
Biological Activity for CGP 20712 dihydrochloride
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 for CGP 20712 dihydrochloride
| M. Wt | 567.39 |
| Formula | C23H25F3N4O5.2HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥96% (HPLC) |
| CAS Number | 1216905-73-5 |
| PubChem ID | 56972164 |
| InChI Key | PURFQCFKYNMIQF-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CN1C=C(N=C1C1=CC=C(OCC(O)CNCCOC2=CC=C(O)C(=C2)C(N)=O)C=C1)C(F)(F)F |
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.
Solubility Data for CGP 20712 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 24.72 | 50 |
Preparing Stock Solutions for CGP 20712 dihydrochloride
The following data is based on the product molecular weight 567.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.52 mL | 17.62 mL | 35.25 mL |
| 2.5 mM | 0.7 mL | 3.52 mL | 7.05 mL |
| 5 mM | 0.35 mL | 1.76 mL | 3.52 mL |
| 25 mM | 0.07 mL | 0.35 mL | 0.7 mL |
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Product Datasheets for CGP 20712 dihydrochloride
References for CGP 20712 dihydrochloride
References are publications that support the biological activity of the product.
Dooley et al (1986) CGP 20712A: a useful tool for quantitating β1- and β2-adrenoceptors. Eur.J.Pharmacol. 130 137 PMID: 2877892
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
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16 Citations for CGP 20712 dihydrochloride
Citations are publications that use Tocris products. Selected citations for CGP 20712 dihydrochloride include:
Ardestani et al (2017) 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. Neuropharmacology 116 371 PMID: 28089846
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
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
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
Lavine et al (2013) Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism. JAMA Ophthalmol 131 376 PMID: 23303344
Lavine (2017) β2-Adrenergic Receptor Antagonism Attenuates CNV Through Inhibition of VEGF and IL-6 Expression. Invest Ophthalmol Vis Sci 58 299 PMID: 28114591
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
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
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
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
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
Creed et al (2015) β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion. Breast Cancer Res 17 145 PMID: 26607426
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
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
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
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.