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    Nebivolol (R 065824)
    Nebivolol (R 065824)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1112
    CAS #: 118457-14-0Purity ≥98%

    Description: Nebivolol (R065824; R-065824; Nobiten; Vasoxen) is a potent and selective beta1/β1-adrenoceptor antagonist with antihypertensive effects. It inhibits β1-adrenoceptor with an IC50 of 0.8 nM. As a beta blocker, nebivolol has been used to treat high blood pressure and heart failure. 

    References: Mol Pharmacol. 1988 Dec;34(6):843-51; Circ J. 2008 Apr;72(4):660-70.

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    Molecular Weight (MW)441.9 
    FormulaC22H25F2NO4.HCl 
    CAS No.152520-56-4 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 88 mg/mL (199.1 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 1-((R)-6-fluorochroman-2-yl)-2-(((R)-2-((R)-6-fluorochroman-2-yl)-2-hydroxyethyl)amino)ethanol

    InChi Key: KOHIRBRYDXPAMZ-JJTQDJFQSA-N

    InChi Code: InChI=1S/C22H25F2NO4/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/t17-,18?,21-,22-/m1/s1

    SMILES Code: O[[email protected]](CNCC([[email protected]]1CCC2=CC(F)=CC=C2O1)O)[[email protected]]3CCC4=CC(F)=CC=C4O3

    SynonymsR-65824; Nebivolol; R 065824; R065824; Nobiten; Vasoxen


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    In Vitro

    In vitro activity: Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (Ki value = 0.9 nM and beta 2/beta 1 ratio = 50). Nebivolol displays β1-adrenoceptor selectivity with the Ki(β2)/Ki(β1) value of 40.7 judged by competition experiments to 3H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, Kiβ2) or ICI 118.551 (50 nM, Kiβ1). Nebivolol reduces cell proliferation of human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Nebivolol treatment for 7 days causes significant reduction in cell growth of haCSMCs with IC50 of 6.1 μM, and inhibits accelerated haCSMC proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ with IC50 values of 6.8 μM, 6.4 μM and 7.7 μM, repectively. Nebivolol treatment (10-5 M) of haCSMCs for 48 hours induces a moderate apoptosis of 23% and a decrease from 16% to 5% in the number of cells in S-phase. During Nebivolol incubation, NO formation of HaCEs increases, while endothelin-1 transcription and secretion are suppressed.


    Cell Assay: Cells [Human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs)] are exposed to different concentrations of Nebivolol (10-7~10-5 M) for 1, 2, 4, 7 and 14 days. Cell proliferation is analyzed by bromodeoxyuridine (BrdU) incorporation, and cell apoptosis is detected by PI or annexin V staining.

    In VivoAdministratiion of Nebivolol (initially by iv within 10 minutes of reperfusion and then orally) to rats with myocardial infarction (MI) reduces myocardial apoptosis, which is mediated by regulation of NO . Nebivolol, significantly, prevents left ventricular (LV) pressure changes, reduces total and regional apoptotic cardiomyocytes. Nebivolol treatment lowers mean blood pressure (MBP) in rats with MI slightly, but not significantly. 
    Animal modelMale Sprague Dawley rat myocardial infarction (MI) model 
    Formulation & DosageDissolved in DMSO and diluted in saline; 2.0 mg/kg; Gastric gavage once daily 
    References

    Mol Pharmacol. 1988 Dec;34(6):843-51; Circ J. 2008 Apr;72(4):660-70. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     
    Nebivolol
    Effects of nebivolol on left ventricular fibrosis and heart function after MI. PLoS One. 2014; 9(5): e98179.
     
    Nebivolol
    Nebivolol administration decreased cardiomyocyte apoptosis. PLoS One. 2014; 9(5): e98179.
     Nebivolol
    Nebivolol administration altered the phosphorylation status of eNOS and increased the expression of nNOS. PLoS One. 2014; 9(5): e98179.


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