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Merck
CN

B2185

Bisoprolol hemifumarate salt

≥98% (HPLC), β1-adrenoceptor antagonist, solid

Synonym(s):

1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol hemifumarate salt

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About This Item

Empirical Formula (Hill Notation):
C18H31NO4 · .5C4H4O4
CAS Number:
104344-23-2
Molecular Weight:
383.48
UNSPSC Code:
12352200
PubChem Substance ID:
24724414
NACRES:
NA.77
MDL number:
MFCD00792743

Key Documents

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Product Name

Bisoprolol hemifumarate salt, ≥98% (HPLC), solid

SMILES string

OC(=O)\C=C\C(O)=O.CC(C)NCC(O)COc1ccc(COCCOC(C)C)cc1.CC(C)NCC(O)COc2ccc(COCCOC(C)C)cc2

InChI key

VMDFASMUILANOL-WXXKFALUSA-N

InChI

1S/2C18H31NO4.C4H4O4/c2*1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4;5-3(6)1-2-4(7)8/h2*5-8,14-15,17,19-20H,9-13H2,1-4H3;1-2H,(H,5,6)(H,7,8)/b;;2-1+

assay

≥98% (HPLC)

form

solid

color

white

solubility

DMSO: >20 mg/mL

originator

Teva

Quality Level

100

Gene Information

human ... ADRB1(153)

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Application

Bisoprolol hemifumarate salt has been used as a β-adrenergic receptor (β-AR) antagonist in cardiac fibrosis mice model.

Biochem/physiol Actions

Bisoprolol hemifumarate is useful in oral formulations due to its high bioavailability. It also shows long elimination half-life.
Cardioselective β1-adrenoceptor antagonist.

Features and Benefits

This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Teva. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

pictograms

Health hazardExclamation mark
GHS08,GHS07

signalword

Warning

Hazard Classifications

Acute Tox. 4 Oral - Repr. 2 - STOT RE 2

target_organs

Heart

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

Regulatory Information

监管及禁止进口产品
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Certificates of Analysis (COA)

Lot/Batch Number
0000360649
0000349370
0000349370
0000360649
0000139510

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Cardiac beta-adrenergic receptor activation mediates distinct and cell type-dependent changes in the expression and distribution of connexin 43
Zhang Y, et al.
Journal of Cellular and Molecular Medicine (2020)
Pharmacokinetics and metabolism of bisoprolol enantiomers in humans
Horikiri Y, et al.
Journal of Pharmaceutical Sciences, 87(3), 289-294 (1998)
A E Tattersfield et al.
British journal of clinical pharmacology, 18(3), 343-347 (1984-09-01)
Bisoprolol is a new beta-adrenoceptor antagonist which has shown beta-adrenoceptor selectivity in studies in isolated tissues. Bronchial and cardiac beta-adrenoceptor blockade were assessed in eight normal subjects before and after oral ingestion of placebo, bisoprolol 20 and 40 mg, metoprolol
Akira Sezai et al.
The Journal of thoracic and cardiovascular surgery, 144(5), 1241-1248 (2012-08-04)
We previously performed a trial of intravenous landiolol hydrochloride during and after cardiac surgery (the PASCAL trial) and demonstrated a preventive effect on postoperative atrial fibrillation (AF). In the present study, we investigated the efficacy of increasing the dose and
Huichao Chang et al.
Journal of pharmaceutical and biomedical analysis, 71, 104-110 (2012-09-06)
A sensitive, specific liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was established for the quantitative determination of amlodipine and bisoprolol, using clenbuterol as the internal standard (IS). The analytes and IS were isolated from 100μL plasma samples by a simple liquid-liquid
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