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CGP 20712 A

  Cat. No.:  DC28121   Featured
Chemical Structure
105737-62-0
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Field of application
CGP 20712 A (CGP 20712 mesylate) is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 A exhibits ~10,000-fold selectivity over β2-adrenoceptors.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 105737-62-0
Chemical Name: CGP 20712A
Synonyms: (±)-2-Hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl]phenoxy]propyl] amino]ethoxy]-benzamide methanesulfonate salt;2-hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenoxy]propyl]amino]ethoxy]benzamide,methanesulfonic acid;CGP-20712A methanesulfonate salt;CGP 20712 DIHYDROCHLORIDE;1-[2-((3-CARBAMOYL-4-HYDROXY)PHENOXY)ETHYLAMINO]-3-[4-(1-METHYL-4-TRIFLUOROMETHYL-2-IMIDAZOLYL)PHENOXY]-2-PROPANOL DIHYDROCHLORIDE;CGP 20712A
SMILES: CS(=O)(O)=O.OC(COC1C=CC(C2=NC(C(F)(F)F)=CN2C)=CC=1)CNCCOC1C=CC(O)=C(C(=O)N)C=1
Formula: C24H29F3N4O8S
M.Wt: 590.569275617599
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: CGP 20712 A (CGP 20712 mesylate) is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 A exhibits ~10,000-fold selectivity over β2-adrenoceptors[1].
Target: IC50: 0.7 nM (β1-adrenoceptor)[1]
In Vivo: Pretreatment of 8-day-old rats with 5 mg/kg CGP 20712 A do not change the plasma ACTH response to insulin injection[3].
In Vitro: In myocytes, the activation of adenylate cyclase causes by β2-adrenoceptors is not detected in the presence of 10 nM, 100 nM or 1000 nM CGP 20712 A (CGP 20712 mesylate), which selectively antagonized beta1-adrenoceptors[2].
References: [1]. Dooley DJ, et al. CGP 20712 A: a useful tool for quantitating beta 1- and beta 2-adrenoceptors. Eur J Pharmacol. 1986 Oct 14;130(1-2):137-9. [2]. Kitagawa Y, et al. Determination of beta-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective beta-antagonists. Br J Pharmacol. 1995 Sep;116(1):1635-43. [3]. Grino M, et al. Ontogeny of insulin-induced hypoglycemia stimulation of adrenocorticotropin secretion in the rat: role of catecholamines. Endocrinology. 1992 Dec;131(6):2763-8.
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