CGP 20712 A
CGP 20712 A Basic information
- Product Name:
- CGP 20712 A
- Synonyms:
-
- CGP 20712A METHANESULFONATE SELECTIVE B1 ADRENOCE
- 1-(2-((3-Carbamoyl-4-hydroxy)phenoxy)ethylamino)-3-(4-(1-methyl-4-trifluoromethyl-2-imidazolyl)phenoxy)-2-propanoldihyd
- CGP207122HCl
- CGP-20712A methanesulfonate salt
- (±)-2-Hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl]phenoxy]propyl] amino]ethoxy]-benzamide methanesulfonate salt
- 1-[2-((3-CARBAMOYL-4-HYDROXY)PHENOXY)ETHYLAMINO]-3-[4-(1-METHYL-4-TRIFLUOROMETHYL-2-IMIDAZOLYL)PHENOXY]-2-PROPANOL DIHYDROCHLORIDE
- CGP 20712 DIHYDROCHLORIDE
- (+/-)-1-(2-(3-carbamoyl-4-hydroxyphenoxy)ethylamino)-3-(4-(1-methyl-4-trifluoromethyl-2-imidazolyl)-phenoxy)-2-propanol methane sulfonate
- CAS:
- 105737-62-0
- MF:
- C24H29F3N4O8S
- MW:
- 590.57
- Product Categories:
-
- Adrenoceptor
- Mol File:
- 105737-62-0.mol
CGP 20712 A Chemical Properties
- storage temp.
- 2-8°C
- solubility
- H2O: 10 mg/mL
- form
- solid
- color
- white
- Water Solubility
- H2O: >10mg/mL
DMSO: 100mg/mL
CGP 20712 A Usage And Synthesis
Uses
CGP-20712A methanesulfonate salt has been used as a β1-adrenergic receptor antagonist in adult rat ventricular myocytes (ARVM) and rat cardiac fibroblasts. It may also be used as an antagonist for the β1-adrenergic receptor in rat bladder smooth muscles.
Biological Activity
Highly selective and potent β 1 -adrenoceptor antagonist (IC 50 = 0.7 nM). Displays 10,000-fold selectivity over β 2 -adrenoceptors. Also available as part of the β -Adrenoceptor Antagonist Tocriset™ .
Biochem/physiol Actions
CGP-20712A methanesulfonate salt is a selective β1-adrenoceptor antagonist.
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.
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.
CGP 20712 A Supplier
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