CGP 20712 A

Modify Date: 2024-01-05 10:15:38

CGP 20712 A Structure
CGP 20712 A structure
Common Name CGP 20712 A
CAS Number 105737-62-0 Molecular Weight 590.56900
Density N/A Boiling Point 764.8ºC at 760mmHg
Molecular Formula C24H29F3N4O8S Melting Point N/A
MSDS Chinese USA Flash Point 416.3ºC

 Use of CGP 20712 A


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].

 Names

Name CGP-20712A methanesulfonate salt
Synonym More Synonyms

 CGP 20712 A Biological Activity

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].
Related Catalog
Target

IC50: 0.7 nM (β1-adrenoceptor)[1]

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].
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].
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.

 Chemical & Physical Properties

Boiling Point 764.8ºC at 760mmHg
Molecular Formula C24H29F3N4O8S
Molecular Weight 590.56900
Flash Point 416.3ºC
Exact Mass 590.16600
PSA 194.61000
LogP 3.99470
Vapour Pressure 9.69E-23mmHg at 25°C
Storage condition 2-8°C

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport
WGK Germany 3

 Articles2

More Articles
CGP 20712 A: a useful tool for quantitating beta 1- and beta 2-adrenoceptors.

Eur. J. Pharmacol. 130 , 137-139, (1986)

CGP 20712 A (1-[2-((3-carbamoyl-4-hydroxy)phenoxy)ethylamino]-3- [4-(1-methyl-4-trifluoromethyl-2-imidazolyl) phenoxy]-2-propanol methanesulfonate), a specific beta 1-adrenoceptor antagonist, was test...

Beta-adrenoceptor subtypes in human coronary artery: desensitization of beta 2-adrenergic vasorelaxation by chronic beta 1-adrenergic stimulation in vitro.

J. Cardiovasc. Pharmacol. 25 , 134-141, (1995)

We previously demonstrated that right atrial strips from patients treated with beta 1-selective antagonists exhibit sensitization of beta 2-adrenergic responses in vitro. We also showed that cardiac b...

 Synonyms

2-hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenoxy]propyl]amino]ethoxy]benzamide,methanesulfonic acid