Nebivolol HCl
For research use only. Not for use in humans.
Catalog No.S1549 Synonyms: R-65824
1 publication
Molecular Weight(MW): 441.9
Nebivolol HCl selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
Selleck's Nebivolol HCl has been cited by 1 publication
Purity & Quality Control
Choose Selective Adrenergic Receptor Inhibitors
Biological Activity
| Description | Nebivolol HCl selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM. | |||||||||||||||||||||||
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| Features | A highly cardioselective compound under certain conditions. | |||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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
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Solubility (25°C)
| In vitro | DMSO | 88 mg/mL (199.14 mM) |
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| 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 |
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| Formula | C22H25F2NO4.HCl |
| CAS No. | 152520-56-4 |
| Storage | powder |
| in solvent | |
| Synonyms | R-65824 |
| Smiles | Cl.OC(CNCC(O)C1CCC2=C(O1)C=CC(=C2)F)C3CCC4=CC(=CC=C4O3)F |
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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 |
| NCT01522950 | Completed | Drug: Nebivolol|Drug: atenolol|Drug: placebo | Hypertension | University of Minnesota - Clinical and Translational Science Institute|Forest Laboratories | May 2010 | Phase 2 |
| NCT01057251 | Completed | Drug: Nebivolol|Drug: Placebo | Hypertension | Forest Laboratories | March 2010 | Phase 4 |
| NCT01077661 | Completed | Drug: Nebivolol | Hypertension|Heart Failure | GlaxoSmithKline | October 2009 | -- |
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