CGP 20712 dihydrochloride

Cat. No. 1024 16 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Highly potent and selective β₁ antagonist

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

纯度： ≥96% (HPLC)

引用文献 (16)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 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.

技术数据 for CGP 20712 dihydrochloride

分子量	567.39
公式	C₂₃H₂₅F₃N₄O₅.2HCl
储存	Desiccate at +4°C
纯度	≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for CGP 20712 dihydrochloride

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	water	24.72	50

制备储备液 for CGP 20712 dihydrochloride

以下数据基于产品分子量 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.

浓度/溶剂体积/质量	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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产品说明书 for CGP 20712 dihydrochloride

分析证书/产品说明书

化学品安全技术说明书

参考文献 for CGP 20712 dihydrochloride

参考文献是支持产品生物活性的出版物。

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

If you know of a relevant reference for CGP 20712 dihydrochloride, please let us know.

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16 篇 CGP 20712 dihydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 CGP 20712 dihydrochloride 的部分引用包括：

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

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

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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