Nebivolol hydrochloride (R-65824)

Catalog No.S1549 Synonyms: R-65824 hydrochloride

For research use only.

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

Nebivolol hydrochloride (R-65824) Chemical Structure

CAS No. 152520-56-4

Selleck's Nebivolol hydrochloride (R-65824) has been cited by 4 Publications

Purity & Quality Control

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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

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 M4PWdGZ2dmO2aX;uJIF{e2G7 NWjLVJRWUW6qaXLpeIlwdiCxZjDyZZBq\CCmZXzhfYVlKGmwd3Hy[EBz\WO2aX\5bY5oKHCxdHHzd4l2dSCldYLy[Y51KCiLS4KpJIlvKEOqaX7ld4UhcGGvc4TldkBwfmG{eTCoR2hQMSCNMTDj[YxteyC|dHHicJkh\XiycnXzd4lv\yCqRWLHJI1m[XO3cnXkJJV{cW6pIFnvcndwemu|IGH1ZZR1em9iYYX0c41ifGWmIIDheINpKGOuYX3wJJBt[XSob4LtMEBKSzVyPU[uN|A6PTdizszN MnXiNlUxQDd5NUO=
HEK293 cells NXzZbFRJTnWwY4Tpc44h[XO|YYm= NFLTNmZKdmirYnn0bY9vKG:oIH\hd5Qhe2:maYXtJIN2enKnboSgLGlP[SliaX6gTGVMOjl|IHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghcHWvYX6gUoF3OS53IH3lZZN2emWmIIXzbY5oKEmxbmfvdot{KFG3YYT0do8h[XW2b33heIVlKHCjdHPoJINt[W2yIIDsZZRnd3KvLDDJR|UxRTdwOUSzNlgh|ryP NXexSoF1OjVyOEe3OVM>
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 (from reference)

Cell Research:

[3]

  • 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.

Animal Research:

[4]

  • Animal Models: Male Sprague Dawley rat myocardial infarction (MI) model
  • Dosages: 2.0 mg/kg
  • Administration: Gastric gavage once daily

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 441.9
Formula

C22H25F2NO4.HCl

CAS No. 152520-56-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC2=C(C=CC(=C2)F)OC1C(CNCC(C3CCC4=C(O3)C=CC(=C4)F)O)O.Cl

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04888728 Completed Drug: DWN12088|Drug: Nebivolol|Drug: Paroxetine 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 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 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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