A potent β-AR antagonist; selective for β1-ARs over β2-ARs (Kis = 25 and 480 nM

Bisoprolol (fumarate) – 100 mg

Brand:
Cayman
CAS:
105878-43-1
Storage:
-20
UN-No:
Non-Hazardous - /

Bisoprolol is a potent β-adrenergic receptor (β-AR) antagonist that is selective for β1-ARs over β2-ARs (Kis = 25 and 480 nM, respectively in S49 cells overexpressing the human receptors).{39505} It also selectively binds to β1-ARs over β2-ARs in human myocardium (Kis = 75.8 and 991 nM, respectively).{39506} Bisoprolol binds to rat ventricular myocytes and heart membrane (Kis = 20 and 38.1 nM, respectively) and to rat β1-AR in salivary glands and β2-AR in reticulocytes (Kis = 24 and 1,945 nM, respectively).{39507,39508} In vivo, it inhibits increases in heart rate induced by isoproterenol (Item No. 15592) in guinea pigs.{39509} Bisoprolol (0.3 mg/kg) inhibits isoproterenol-induced increases in heart rate and myocardial contractility in conscious dogs. It also decreases blood pressure and heart rate in spontaneously hypertensive rats (SHRs) when chronically administered at a dose of 7.5 mg/kg twice per day over 19 weeks. Formulations containing bisoprolol have been used in the treatment of heart failure, angina pectoris, mild to moderate hypertension, and for secondary prevention of myocardial infarction.  

 

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SKU: 23827 - 100 mg Category:

Description

A potent β-AR antagonist; selective for β1-ARs over β2-ARs (Kis = 25 and 480 nM, respectively in S49 cells overexpressing the human receptors); inhibits isoproterenol-induced increases in heart rate in guinea pigs; inhibits isoproterenol-induced increases in heart rate and myocardial contractility in conscious dogs (0.3 mg/kg); decreases blood pressure and heart rate in SHRs (7.5 mg/kg twice per day over 19 weeks),

Formal name: 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol, (2E)-2-monobutenedioate

Synonyms:  EMD 33512

Molecular weight: 441.5

CAS: 105878-43-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Blood|Erythrocytes & Hemoglobin||Research Area|Cardiovascular System|Cardiovascular Diseases|Angina||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Heart|Myocardial Contractility

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