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经验公式(希尔记法):
C23H25F3N4O5 · CH4O3S
化学文摘社编号:
分子量:
590.57
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
CGP-20712A methanesulfonate salt, solid, ≥98% (HPLC)
SMILES string
CS(O)(=O)=O.Cn1cc(nc1-c2ccc(OCC(O)CNCCOc3ccc(O)c(c3)C(N)=O)cc2)C(F)(F)F
InChI key
VFPOVCXWKBYDNF-UHFFFAOYSA-N
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)
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
Quality Level
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.
Disclaimer
Product is hygroscopic
Legal Information
Sold exclusively with the permission of Ciba-Geigy.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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
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
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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