Home Neuronal Signaling Adrenergic Receptor antagonist Nebivolol hydrochloride (R-65824) For research use only.

Nebivolol hydrochloride (R-65824)

Synonyms: R-65824 hydrochloride

Nebivolol HCl (R-65824) selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.

Nebivolol hydrochloride (R-65824) Chemical Structure

Nebivolol hydrochloride (R-65824) Chemical Structure

CAS No. 152520-56-4

Purity & Quality Control

Nebivolol hydrochloride (R-65824) Related Products

Signaling Pathway

Adrenergic Receptor Signaling Pathways

Adrenergic Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
(CHO) K1 cells Function assay Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform, IC50=6.30957 μM 25087753
HEK293 cells Function assay Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50=7.94328 μM 25087753
Click to View More Cell Line Experimental Data

Biological Activity

Description Nebivolol HCl (R-65824) 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
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 Research 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.
In Vivo
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]
Animal Research Animal Models Male Sprague Dawley rat myocardial infarction (MI) model
Dosages 2.0 mg/kg
Administration Gastric gavage once daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06004453 Recruiting
Heart Failure
Novartis Pharmaceuticals|Novartis
 April 4 2023 --
NCT04888728 Completed
Idiopathic Pulmonary Fibrosis
Daewoong Pharmaceutical Co. LTD.
 June 30 2021 Phase 1
NCT03847350 Completed
Essential Hypertension
A.Menarini Asia-Pacific Holdings Pte Ltd
 July 1 2015 --
NCT01885988 Unknown status
Erectile Dysfunction
Martin M. Miner MD|Forest Laboratories|The Miriam Hospital
 March 2013 Phase 4
NCT01057251 Completed
Hypertension
Forest Laboratories
 March 2010 Phase 4

Chemical Information & Solubility

Molecular Weight 441.9 Formula

C22H25F2NO4.HCl
CAS No. 152520-56-4 SDF Download Nebivolol hydrochloride (R-65824) SDF
Smiles C1CC2=C(C=CC(=C2)F)OC1C(CNCC(C3CCC4=C(O3)C=CC(=C4)F)O)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (199.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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