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104344-23-2 ((±)-Bisoprolol (hemifumarate))

1

Identification

(±)-Bisoprolol (hemifumarate) (±)-Bisoprolol (hemifumarate)
Name (±)-Bisoprolol (hemifumarate)
Formula C40H66N2O12
MW 766.96
CAS No. 104344-23-2
EINECS
Smiles OC(CNC(C)C)COC1=CC=C(COCCOC(C)C)C=C1.OC(CNC(C)C)COC2=CC=C(COCCOC(C)C)C=C2.OC(/C=C/C(O)=O)=O
Synonyms Bisoprolol hemifumarate salt; 1-(4-((2-isopropoxyethoxy)methyl)phenoxy)-3-(isopropylamino)propan-2-ol hemifumarate
InChI 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+
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Introduction

Bisoprolol is a selective type β1 adrenergic receptor blocker. Target: Adrenergic Receptor Approved: July 31, 1992 Bisoprolol, on beta 1-adrenoceptor peptide induced autoimmune myocardial damage.

Background Information

Bisoprolol fumarate is a selective type β1 adrenergic receptor blocker. ......by AbMole BioScience
Bisoprolol is a beta-adrenoceptor blocking drug (beta-blocker). More specifically, it is a selective type β1 adrenergic receptor blocker. ......by BOC Sciences
Bisoprolol hemifumarate is a cardioselective beta-1 adrenergic blocker. It is effective in the management of hypertension and angina pectoris. Bisoprolol hemifumarate has antihypertensive and potential cardioprotective activities. Devoid of intrinsic sympathomimetic activity, bisoprolol selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, decreasing cardiac contractility and rate, reducing cardiac output, and lowering blood pressure. ......by MedKoo Biosciences, Inc.
A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. ......by Target Molecule Corp.
A selective β1-adrenergic antagonist. Has a Kd of 2-3 nM at the β1 receptor and a β1/β2 selectivity of approximately 100-fold. ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000013243

Storage condition

Store at RT by Tocris Bioscience Inc.

Solubility

DMSO 88 mg/mL Water 88 mg/mL Ethanol 88 mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 88 mg/mL (199.31 mM); Water88 mg/mL (199.31 mM); Ethanol88 mg/mL (199.31 mM) by Selleck Chemicals LLC
Soluble to 50 mM in water by Tocris Bioscience Inc.
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Mechanism and Indication

Signaling Pathways GPCR/G Protein
Target Adrenergic Receptor
Research Area Inflammation/Immunology
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
(±)-Bisoprolol (hemifumarate) - Launched
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Safety Data of (±)-Bisoprolol (hemifumarate)

Hazard Symbols : Xn,Xi
Risk Statements : 22
RTECS : UB8390000
WGKGermany : 3
8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AA Blocks LLC
AbMole BioScience USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BLD Pharmatech
BOC Sciences
Beijing Eagle Sky Pharmatech Co., Ltd. China
Beijing Gaobo Pharm-Chemicals Tech. Co., Ltd CHINA
Beijing Mesochem Technology Co., Ltd. China
Biochempartner Co., Ltd China
CHEMSCENE, LLC 100mg/USD82();200mg/USD119() USA
Hanzhong Hanjiang-Venturepharm Pharmaceutical Ltd. China
MedChemexpress Co., Ltd. 100mg/USD82();200mg/USD119() USA
MedKoo Biosciences, Inc. USA
Selleck Chemicals LLC 25mg/USD100(In stock);10mM/1mLIn DMSO/USD220(In stock);100mg/USD350(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 100mg/USD82();200mg/USD119() China
Target Molecule Corp. 2mg/USD24();10mg/USD98();25mg/USD156();100mg/USD198() USA
Tocris Bioscience Inc. USA
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Related Products

Other Forms of 104344-23-2

Name CAS No Formula MW

Recommended Compounds in Adrenergic Receptor

Name CAS No Formula MW
Tolazoline 59-98-3 C10H12N2 160.22
Synephrine (hydrochloride) 5985-28-4 C9H14ClNO2 203.67
(R)-(-)-Phenylephrine 59-42-7 C9H13NO2 167.205
Nicergoline 27848-84-6 C24H26BrN3O3 484.39
Tamsulosin (hydrochloride) 106463-17-6 C20H29ClN2O5S 444.97
Tamsulosin 106133-20-4 C20H28N2O5S 408.51
UK 14,304 59803-98-4 C11H10BrN5 292.13
Guanfacine 29110-47-2 C9H9Cl2N3O 246.09
Propranolol (hydrochloride) 318-98-9 C16H22ClNO2 295.8
Guanabenz (Acetate) 23256-50-0 C10H12Cl2N4O2 291.13
Tetrahydrozoline (hydrochloride) 522-48-5 C13H17ClN2 236.74
Octopamine (hydrochloride) 770-05-8 C8H12ClNO2 189.64
Betaxolol (hydrochloride) 63659-19-8 C18H30ClNO3 343.89
Indacaterol (maleate) 753498-25-8 C28H32N2O7 508.56
Medetomidine (hydrochloride) 86347-15-1 C13H17ClN2 236.74
Norepinephrine (bitartrate monohydrate) 108341-18-0 C12H19NO10 337.28
Norepinephrine (hydrochloride) 329-56-6 C8H12ClNO3 205.64
Xylometazoline (hydrochloride) 1218-35-5 C16H25ClN2 280.84
(R)-(-)-Phenylephrine (hydrochloride) 61-76-7 C9H14ClNO2 203.67
Isoprenaline (hydrochloride) 51-30-9 C11H18ClNO3 247.72

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

[1]. Matsui, S., et al., Protective effect of bisoprolol on beta-1 adrenoceptor peptide-induced autoimmune myocardial damage in rabbits. Herz, 2000. 25(3): p. 267-70.

[2]. Wargon, M., et al., Acute effects of bisoprolol on respiratory sinus arrhythmia. Fundam Clin Pharmacol, 1998. 12(4): p. 451-6.

Protocol Reference

Kaumann and Lemoine (1985) Direct labelling of myocardial β1-adrenoceptors. Comparison of binding affinity of 3H-(-)-bisoprolol with its blocking potency. Naunyn Schmiedebergs Arch.Pharmacol. 331 27. PMID: 2866449.

Klockow et al (1986) Studies on the receptor profile of bisoprolol. Arzneimittelforschung 36 197. PMID: 2870719.

Heible et al (1995) α-and β-Adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J.Med.Chem. 38 3415. PMID: