A β1-AR antagonist
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Nebivolol (hydrochloride)

Item No. 23660

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αR,α'R,2R,2'S)-rel-α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol, monohydrochloride
CAS Number
152520-56-4
Molecular Formula
C22H25F2NO4 • HCl
Formula Weight
441.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 30 mg/mlEthanol: 0.5 mg/ml
λmax
281 nm
SMILES
FC1=CC=C2C(CC[C@]([C@@H](O)CNC[C@H](O)[C@@]3([H])CCC(C=C(F)C=C4)=C4O3)([H])O2)=C1.Cl
InChi Code
InChI=1S/C22H25F2NO4.ClH/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22;/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2;1H/t17-,18-,21-,22+;/m0./s1
InChi Key
JWEXHQAEWHKGCW-BIISKSHESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $41

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    10 mg

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    25 mg

    $128

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    50 mg

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    Product Description

    Nebivolol is an antagonist of the β1-adrenergic receptor (β1-AR; IC50 = 7.41 nM).1 It is selective for β1- over β2-ARs (IC50 = 251 nM), as well as the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2 and the α1- and α2-adrenergic, histamine H1, and dopamine D2 receptors (IC50s = 27.5, 2,239, 3,162, >10,000, 5,623, and 10,000 nM, respectively). Nebivolol induces vasodilation in isolated mouse renal arteries (EC50 = 11.36 μM) and decreases contraction of isolated human left ventricular trabeculae induced by isoproterenol (Item No. 15592; IC50 = 7 μM).2,3 Nebivolol inhibits proliferation of primary human coronary artery smooth muscle cells (HCASMCs) in the presence and absence of growth factors (IC50s = 6.1, 6.8, 6.4, and 7.7 μM for HCASMCs grown in media containing no growth factor, PDGF-BB, basic FGF, and TGF-β1, respectively).4 It is also an inhibitor of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), also known as 3C-like protease (3CLpro; IC50 = 60.2 µg/ml), and inhibits SARS-CoV-2 pathogenicity in vitro (IC50 = 0.03 µg/ml).5 Formulations containing nebivolol have been used in the treatment of hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pauwels, P.J., Gommeren, W., Van Lommen, G., et al. The receptor binding profile of the new antihypertensive agent nebivolol and its stereoisomers compared with various β-adrenergic blockers. Mol. Pharmacol. 34(6), 843-851 (1988).

    2. Georgescu, A., Pluteanu, F., Flonta, M.L., et al. Nebivolol induces a hyperpolarizing effect on smooth muscle cells in the mouse renal artery by activation of beta-2-adrenoceptors. Pharmacology 81(2), 110-117 (2008).

    3. Brixius, K., Bundkirchen, A., Bölck, B., et al. Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardium. Br. J. Pharmacol. 133(8), 1330-1338 (2001).

    4. Brehm, B.R., Wolf, S.C., Bertsch, D., et al. Effects of nebivolol on proliferation and apoptosis of human coronary artery smooth muscle and endothelial cells. Cardiovasc. Res. 49(2), 430-439 (2001).

    5. Hamed, M.I.A., Darwish, K.M., Soltane, R., et al. β-Blockers bearing hydroxyethylamine and hydroxyethylene as potential SARS-CoV-2 Mpro inhibitors: Rational based design, in silico, in vitro, and SAR studies for lead optimization. RSC Adv. 11(56), 35536-35558 (2021).