C231

Sigma-Aldrich

CGP-20712A methanesulfonate salt

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
Empirical Formula (Hill Notation):
C23H25F3N4O5 · CH4O3S
CAS Number:
Molecular Weight:
590.57
MDL number:
PubChem Substance ID:
NACRES:
NA.77
Pricing and availability is not currently available.

Quality Level

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.

Packaging

10, 50 mg in glass bottle

Biochem/physiol Actions

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

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

Caution

Product is hygroscopic

Legal Information

Sold exclusively with the permission of Ciba-Geigy.
LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Personal Protective Equipment

dust mask type N95 (US),Eyeshields,Gloves

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis
Certificate of Origin
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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