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C231

CGP-20712A methanesulfonate salt

Name: CGP-20712A methanesulfonate salt
Brand: SIGMA

solid, ≥98% (HPLC)

Synonym(e):

(±)-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

Empirische Formel (Hill-System):

C₂₃H₂₅F₃N₄O₅ · CH₄O₃S

CAS-Nummer:

105737-62-0

Molekulargewicht:

590.57

MDL-Nummer:

MFCD00798870

UNSPSC-Code:

12352200

PubChem Substanz-ID:

24278787

NACRES:

NA.77

Assay

≥98% (HPLC)

Form

solid

Lagerbedingungen

desiccated

Farbe

white to off-white

Löslichkeit

H₂O: >10 mg/mL
DMSO: 100 mg/mL

Lagertemp.

2-8°C

SMILES String

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)

InChIKey

VFPOVCXWKBYDNF-UHFFFAOYSA-N

Angaben zum Gen

human ... ADRB1(153)

Anwendung

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.

Biochem./physiol. Wirkung

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

Vorsicht

Product is hygroscopic

Rechtliche Hinweise

Sold exclusively with the permission of Ciba-Geigy.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

Eyeshields, Gloves, type N95 (US)

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

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

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

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

Intestinal anti-inflammatory effects of total alkaloid extract from Fumaria capreolata in the DNBS model of mice colitis and intestinal epithelial CMT93 cells.

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.

β-Adrenergic regulation of cardiac type 2A protein phosphatase through phosphorylation of regulatory subunit B56δ at S573.

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

O-GlcNAc transferase affects the signal transduction of β1 adrenoceptor in adult rat cardiomyocytes by increasing the O-GlcNAcylation of β1 adrenoceptor.

Hong Cao et al.

Biochemical and biophysical research communications, 528(1), 71-77 (2020-05-31)

O-GlcNAcylation was first found by Torres and Hart in monocytes. It is a dynamic and reversible post-translational modification catalyzed by O-GlcNAc transferase (OGT) and O-GlcNAcase (OGA). O-GlcNAcylation is increased in diabetic cardiomyopathy (DCM) patients and it has been reported that

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