Nebivolol HCl

Catalog No.S1549 Synonyms: R-65824

Nebivolol HCl Chemical Structure

Molecular Weight(MW): 441.9

Nebivolol HCl selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 60 In stock
USD 170 In stock
USD 370 In stock
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Biological Activity

Description Nebivolol HCl selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
Features A highly cardioselective compound under certain conditions.
Targets
β1-adrenoceptor [1]
0.8 nM
In vitro

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). [1] 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). [2] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
(CHO) K1 cells MVzGeY5kfGmxbjDhd5NigQ>? M17UbWlvcGmkaYTpc44hd2ZicnHwbYQh\GWuYYnl[EBqdnejcnSgdoVkfGmoeXnu[{Bxd3Sjc4PpeY0h[3W{cnXueEApUUu{KTDpckBEcGmwZYPlJIhidXO2ZYKgc5ZienliKFPIU{khUzFiY3XscJMhe3SjYnz5JIV5eHKnc4PpcochcEWURzDt[YF{fXKnZDD1d4lv\yCLb37Xc5JseyCTdXH0eJJwKGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDwcIF1\m:{bTygTWM2OD14LkOwPVU4KM7:TR?= NVrRbZRtOjVyOEe3OVM>
HEK293 cells MVjGeY5kfGmxbjDhd5NigQ>? NGfsbG5KdmirYnn0bY9vKG:oIH\hd5Qhe2:maYXtJIN2enKnboSgLGlP[SliaX6gTGVMOjl|IHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghcHWvYX6gUoF3OS53IH3lZZN2emWmIIXzbY5oKEmxbmfvdot{KFG3YYT0do8h[XW2b33heIVlKHCjdHPoJINt[W2yIIDsZZRnd3KvLDDJR|UxRTdwOUSzNlgh|ryP Mnr0NlUxQDd5NUO=

... Click to View More Cell Line Experimental Data

In vivo Administratiion 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. [4]

Protocol

Cell Research:[3]
+ Expand
  • Cell lines: Human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs)
  • Concentrations: Dissolved in 100% methanol and diluted with three volumes of growth medium to obtain a stock solution of 10-3 M, final concentration 10-7~10-5 M
  • Incubation Time: 1, 2, 4, 7 and 14 days
  • Method: Cells 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.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: Male Sprague Dawley rat myocardial infarction (MI) model
  • Formulation: Dissolved in DMSO and diluted in saline
  • Dosages: 2.0 mg/kg
  • Administration: Gastric gavage once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (199.14 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 441.9
Formula

C22H25F2NO4.HCl

CAS No. 152520-56-4
Storage powder
in solvent
Synonyms R-65824

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03180593 Completed Hypertension Complicated|Hypertrophy Left Ventricular|Blood Pressure Trinity Hypertension & Metabolic Research Institute|Allergan Sales LLC February 7 2017 Phase 4
NCT03635125 Completed JNC 7 Stage 1 or 2 Hypertension Trinity Hypertension & Metabolic Research Institute August 30 2010 Phase 4
NCT03598673 Recruiting Hypertension University of Abuja|Micronova Pharmaceuticals Ind Ltd February 27 2018 --
NCT02619526 Recruiting Heart Failure Dong-A University|Menarini Group December 2016 Not Applicable
NCT02710071 Completed Hypertension University of California San Diego January 2015 Phase 4
NCT01665508 Completed Microvascular Angina Massachusetts General Hospital|Forest Laboratories April 2013 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID