Name: Nebivolol hydrochloride (R-65824)
Brand: Selleck Chemicals
SKU: S1549
Availability: InStock
Rating: 5 (6 reviews)

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Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Adrenergic Receptor Inhibitors	Zenidolol (ICI-118551) Hydrochloride L755507 Yohimbine HCl Atipamezole Higenamine hydrochloride Detomidine HCl Naftopidil Demethyl-Coclaurine Buflomedil HCl Fenoterol hydrobromide

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
(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
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (199.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5% DMSO 1 20% PEG 300 2 5%Tween80 3 70%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.400mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 88 mg/ml clarified DMSO stock solution to 200 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 700 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	441.9	Formula	C₂₂H₂₅F₂NO₄.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	152520-56-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	R-65824 hydrochloride			Smiles	C1CC2=C(C=CC(=C2)F)OC1C(CNCC(C3CCC4=C(O3)C=CC(=C4)F)O)O.Cl

Mechanism of Action

Features	A highly cardioselective compound under certain conditions.
Targets/IC₅₀/Ki	β1-adrenoceptor 0.8 nM
In vitro	Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (K_i value = 0.9 nM and beta 2/beta 1 ratio = 50). Nebivolol displays β1-adrenoceptor selectivity with the K_i(β2)/K_i(β1) value of 40.7 judged by competition experiments to ³H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, K_iβ2) or ICI 118.551 (50 nM, K_iβ1). 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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/2462161/ [2] https://pubmed.ncbi.nlm.nih.gov/11498519/ [3] https://pubmed.ncbi.nlm.nih.gov/11164853/ [4] https://pubmed.ncbi.nlm.nih.gov/18362441/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Nebivolol hydrochloride (R-65824) Adrenergic Receptor antagonist

Chemical Structure

Molecular Weight: 441.9