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C231

Sigma-Aldrich

CGP-20712A methanesulfonate salt

solid, ≥98% (HPLC)

Synonyme(s) :

(±)-2-Hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl]phenoxy]propyl] amino]ethoxy]-benzamide methanesulfonate salt

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About This Item

Formule empirique (notation de Hill):
C23H25F3N4O5 · CH4O3S
Numéro CAS:
105737-62-0
Poids moléculaire :
590.57
Numéro MDL:
MFCD00798870
Code UNSPSC :
12352200
ID de substance PubChem :
24278787
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

solid

Conditions de stockage

desiccated

Couleur

white to off-white

Solubilité

H2O: >10 mg/mL
DMSO: 100 mg/mL

Température de stockage

2-8°C

Chaîne SMILES 

CS(O)(=O)=O.Cn1cc(nc1-c2ccc(OCC(O)CNCCOc3ccc(O)c(c3)C(N)=O)cc2)C(F)(F)F

InChI

1S/C23H25F3N4O5.CH4O3S/c1-30-12-20(23(24,25)26)29-22(30)14-2-4-16(5-3-14)35-13-15(31)11-28-8-9-34-17-6-7-19(32)18(10-17)21(27)33;1-5(2,3)4/h2-7,10,12,15,28,31-32H,8-9,11,13H2,1H3,(H2,27,33);1H3,(H,2,3,4)

Clé InChI

VFPOVCXWKBYDNF-UHFFFAOYSA-N

Informations sur le gène

human ... ADRB1(153)

Application

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.

Actions biochimiques/physiologiques

CGP-20712A methanesulfonate salt is a selective β1-adrenoceptor antagonist.

Attention

Product is hygroscopic

Informations légales

Sold exclusively with the permission of Ciba-Geigy.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

Eyeshields, Gloves, type N95 (US)

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

A Ferro et al.
Journal of cardiovascular pharmacology, 25(1), 134-141 (1995-01-01)
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 beta 2-adrenergic sensitization can be induced in normal subjects prospectively by beta 1-blocker
D J Dooley et al.
European journal of pharmacology, 130(1-2), 137-139 (1986-10-14)
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 tested for resolution of beta 1- and beta 2-adrenoceptors in an in vitro [3H]dihydroalprenolol ([3H]DHA) binding assay. Competition experiments, using rat neocortical and cerebellar membranes, yielded two
Noureddine Bribi et al.
Phytomedicine : international journal of phytotherapy and phytopharmacology, 23(9), 901-913 (2016-07-09)
Fumaria capreolata L. (Papaveraceae) is a botanical drug used in North Africa for its gastro-intestinal and anti-inflammatory properties. It is characterized for the presence of several alkaloids that could be responsible for some of its effects, including an immunomodulatory activity.
Rhonda L Carter et al.
Pharmacology research & perspectives, 2(1) (2014-04-01)
Label-free systems for the agnostic assessment of cellular responses to receptor stimulation have been shown to provide a sensitive method to dissect receptor signaling. β-adenergic receptors (βAR) are important regulators of normal and pathologic cardiac function and are expressed in
Antonella Ranieri et al.
Journal of molecular and cellular cardiology, 115, 20-31 (2018-01-03)
Type 2A protein phosphatase (PP2A) enzymes are serine/threonine phosphatases which comprise a scaffold A subunit, a regulatory B subunit and a catalytic C subunit, and have been implicated in the dephosphorylation of multiple cardiac phosphoproteins. B subunits determine subcellular targeting
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