Bisoprolol (hemifumarate)

Bisoprolol is an antagonist of the beta1-adrenergic receptor (beta1-AR, Ki = 25 nM for the human receptor). It is selective for beta1- over beta2-ARs (Ki = 480 nM for the human receptor in a radioligand binding assay). Bisoprolol binds to rat ventricular myocytes and heart membranes that endogenously express beta1-ARs and beta1- and beta2-ARs, respectively (Kis = 20 and 38.1 nM, respectively). In vivo, bisoprolol (0.3 mg/kg) inhibits increases in heart rate and myocardial contractility induced by isoproterenol (Cay-15592) in conscious dogs. 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). 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.Formal Name: 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol, (2E)-2-butenedioate (2:1). CAS Number: 104344-23-2. Synonyms: EMD 33512. Molecular Formula: C18H31NO4 . 1/2C4H4O4. Formula Weight: 325.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 224 nm. SMILES: OC(CNC(C)C)COC1=CC=C(COCCOC(C)C)C=C1.OC(/C=C/C(O)=O)=OOC(C)C)C=C1.OC(/C=C/C(O)=O)=O. InChi Code: InChI=1S/C18H31NO4.C4H4O4/c1-14(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/h5-8,14-15,17,19-20H,9-13H2,1-4H3,1-2H,(H,5,6)(H,7,8)/b,2-1+. InChi Key: RZPZLFIUFMNCLY-WLHGVMLRSA-N.