Nebivolol HCl
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
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
| Cell Research:[3] |
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| Animal Research:[4] |
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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 |
Bio Calculators
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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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