For research use only.
Catalog No.S1549 Synonyms: R-65824
Molecular Weight(MW): 441.9
Nebivolol HCl selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
Purity & Quality Control
Choose Selective Adrenergic Receptor Inhibitors
|Description||Nebivolol HCl selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.|
|Features||A highly cardioselective compound under certain conditions.|
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. 
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. 
|In vitro||DMSO||88 mg/mL (199.14 mM)|
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03847350||Completed||--||Essential Hypertension||A.Menarini Asia-Pacific Holdings Pte Ltd||July 1 2015||--|
|NCT01885988||Unknown status||Drug: Nebivolol|Drug: Sugar Pill||Erectile Dysfunction||Martin M. Miner MD|Forest Laboratories|The Miriam Hospital||March 2013||Phase 4|
|NCT01057251||Completed||Drug: Nebivolol|Drug: Placebo||Hypertension||Forest Laboratories||March 2010||Phase 4|
|NCT01077661||Completed||Drug: Nebivolol||Hypertension|Heart Failure||GlaxoSmithKline||October 2009||--|
|NCT00999752||Completed||Drug: Nebivolol|Drug: Hydrochlorothiazide||Hypertension||InVasc Therapeutics Inc.||October 2009||Not Applicable|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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