Formulation: A solid
Formal Name: 1-(4-((2-isopropoxyethoxy)methyl)phenoxy)-3-((propan-2-yl-d7)amino)propan-2-ol, hemifumarate
Purity: ≥99% deuterated forms (d1-d7)
Formula Markup: C18H24D7NO4 • 1/2C4H4O4
Formula Weight: 390,5
Shelf life (days): 1460
Notes: Bisoprolol-d7 is intended for use as an internal standard for the quantification of bisoprolol (Item No. 23827) by GC- or LC-MS. Bisoprolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 25 nM for the human receptor).{39505} It is selective for β1- over β2-ARs (Ki = 480 nM for the human receptor in a radioligand binding assay).{39505} Bisoprolol binds to rat ventricular myocytes and heart membranes that endogenously express β1-ARs and β1- and β2-ARs, respectively (Kis = 20 and 38.1 nM, respectively).{39507} In vivo, bisoprolol (0.3 mg/kg) inhibits increases in heart rate and myocardial contractility induced by isoproterenol (Item No. 15592) in conscious dogs.{39509} It 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. Bisoprolol also inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), also known as 3C-like protease (3CLpro; IC50 = 118.5 µg/ml) and reduces viral infectivity in SARS-CoV-2 infected Vero E6 cells (IC50 = 15.917 µg/ml).{64706} 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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