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CGP-20712A methanesulfonate salt

Name: CGP-20712A methanesulfonate salt
Brand: SIGMA

solid, ≥98% (HPLC)

Synonym(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

Empirical Formula (Hill Notation):

C₂₃H₂₅F₃N₄O₅ · CH₄O₃S

CAS Number:

105737-62-0

Molecular Weight:

590.57

MDL number:

MFCD00798870

UNSPSC Code:

12352200

PubChem Substance ID:

24278787

NACRES:

NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

solid

storage condition

desiccated

color

white to off-white

solubility

H₂O: >10 mg/mL
DMSO: 100 mg/mL

storage temp.

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)

InChI key

VFPOVCXWKBYDNF-UHFFFAOYSA-N

Gene Information

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.

Biochem/physiol Actions

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

Caution

Product is hygroscopic

Legal Information

Sold exclusively with the permission of Ciba-Geigy.

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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.

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

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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