Nebivolol HCl | CAS#152520-56-4 | beta1-receptor antagonist

MedKoo Cat#: 562878 | Name: Nebivolol HCl

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Nebivolol HCl is a selective beta1-receptor antagonist.

Chemical Structure

Nebivolol HCl

CAS#152520-56-4

Theoretical Analysis

MedKoo Cat#: 562878

Name: Nebivolol HCl

CAS#: 152520-56-4

Chemical Formula: C22H26ClF2NO4

Exact Mass:

Molecular Weight: 441.90

Elemental Analysis: C, 59.80; H, 5.93; Cl, 8.02; F, 8.60; N, 3.17; O, 14.48

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 240.00
50mg	USD 550.00

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Related CAS #

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Synonym

Nebivolol HCl; Nebivolol Hydrochloride; Silostar; Bystolic, R-67145; R 67145; R67145;

IUPAC/Chemical Name

(R)-1-((R)-6-fluorochroman-2-yl)-2-(((S)-2-((S)-6-fluorochroman-2-yl)-2-hydroxyethyl)amino)ethan-1-ol hydrochloride

InChi Key

JWEXHQAEWHKGCW-FNLXBVDKSA-N

InChi Code

InChI=1S/C22H25F2NO4.ClH/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22;/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2;1H/t17-,18+,21-,22+;

SMILES Code

O[C@@H]([C@H]1CCC2=C(O1)C=CC(F)=C2)CNC[C@H](O)[C@@H]3CCC4=C(O3)C=CC(F)=C4.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Nebivolol (R 065824) hydrochloride is an orally active beta receptor blocker.

In vitro activity:

After 24 h of AA exposure, significantly reduced cell viability and intracellular ROS overproduction were observed in EAhy926 cells; both effects were counteracted by NEB (nebivolol) pretreatment. After 48 h of exposure to AA, the most prominent metabolite changes were significant decreases in arginine, glutamate, glutamine and glutathione levels, along with a significant increase in the aspartate, glycerophosphocholine and UDP-N-acetylglucosamine contents. NEB pretreatment slightly inhibited the changes in glutathione and glycerophosphocholine. Reference: Toxins (Basel). 2022 Feb 10;14(2):132. https://pubmed.ncbi.nlm.nih.gov/35202159/

In vivo activity:

Treatment with nebivolol (10 mg/kg/day; p.o. gavage) prevented the increase of both superoxide (O2•-) and thiobarbituric acid reactive substances (TBARS) in the left ventricle of rats chronically treated with ethanol. Nebivolol prevented ethanol-induced increase of Nox2 expression in the left ventricle. Reference: Cardiovasc Toxicol. 2021 Mar;21(3):224-235. https://pubmed.ncbi.nlm.nih.gov/33067693/

	Solvent	mg/mL	mM
Solubility
	DMF	20.0	45.26
	DMSO	65.6	148.33
	Ethanol	2.5	5.57
	Water	1.8	4.05

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 441.90 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Antoine MH, Husson C, Yankep T, Mahria S, Tagliatti V, Colet JM, Nortier J. Protective Effect of Nebivolol against Oxidative Stress Induced by Aristolochic Acids in Endothelial Cells. Toxins (Basel). 2022 Feb 10;14(2):132. doi: 10.3390/toxins14020132. PMID: 35202159; PMCID: PMC8876861. 2. Chen Q, Jiang H, Wang Z, Cai LY, Jiang YC, Xie L, Zhou Y, Zeng X, Ji N, Shen YQ, Chen QM. Adrenergic Blockade by Nebivolol to Suppress Oral Squamous Cell Carcinoma Growth via Endoplasmic Reticulum Stress and Mitochondria Dysfunction. Front Pharmacol. 2021 Aug 12;12:691998. doi: 10.3389/fphar.2021.691998. PMID: 34456721; PMCID: PMC8387679. 3. do Vale GT, da Silva CBP, Sousa AH, Gonzaga NA, Parente JM, Araújo KM, Castro MM, Tirapelli CR. Nebivolol Prevents Up-Regulation of Nox2/NADPH Oxidase and Lipoperoxidation in the Early Stages of Ethanol-Induced Cardiac Toxicity. Cardiovasc Toxicol. 2021 Mar;21(3):224-235. doi: 10.1007/s12012-020-09614-1. Epub 2020 Oct 16. PMID: 33067693. 4. Oelze M, Daiber A, Brandes RP, Hortmann M, Wenzel P, Hink U, Schulz E, Mollnau H, von Sandersleben A, Kleschyov AL, Mülsch A, Li H, Förstermann U, Münzel T. Nebivolol inhibits superoxide formation by NADPH oxidase and endothelial dysfunction in angiotensin II-treated rats. Hypertension. 2006 Oct;48(4):677-84. doi: 10.1161/01.HYP.0000239207.82326.29. Epub 2006 Aug 28. PMID: 16940222.

In vitro protocol:

In vivo protocol:

1. do Vale GT, da Silva CBP, Sousa AH, Gonzaga NA, Parente JM, Araújo KM, Castro MM, Tirapelli CR. Nebivolol Prevents Up-Regulation of Nox2/NADPH Oxidase and Lipoperoxidation in the Early Stages of Ethanol-Induced Cardiac Toxicity. Cardiovasc Toxicol. 2021 Mar;21(3):224-235. doi: 10.1007/s12012-020-09614-1. Epub 2020 Oct 16. PMID: 33067693. 2. Oelze M, Daiber A, Brandes RP, Hortmann M, Wenzel P, Hink U, Schulz E, Mollnau H, von Sandersleben A, Kleschyov AL, Mülsch A, Li H, Förstermann U, Münzel T. Nebivolol inhibits superoxide formation by NADPH oxidase and endothelial dysfunction in angiotensin II-treated rats. Hypertension. 2006 Oct;48(4):677-84. doi: 10.1161/01.HYP.0000239207.82326.29. Epub 2006 Aug 28. PMID: 16940222.

1: Abdel-Fattah L, Abdel-Aziz L, El-Kosasy A, Gaied M. Quantification of nebivolol hydrochloride in human plasma by liquid chromatography using fluorescence detection: Use in pharmacokinetic study. Drug Discov Ther. 2010 Dec;4(6):418-22. PubMed PMID: 22491307. 2: Hussar DA. New drugs 09, part 1. Plast Surg Nurs. 2009 Oct-Dec;29(4):228-36; quiz 237-8. doi: 10.1097/PSN.0b013e3181d0512c. Review. PubMed PMID: 20029303. 3: Bundkirchen A, Brixius K, Bölck B, Nguyen Q, Schwinger RH. Beta 1-adrenoceptor selectivity of nebivolol and bisoprolol. A comparison of [3H]CGP 12.177 and [125I]iodocyanopindolol binding studies. Eur J Pharmacol. 2003 Jan 26;460(1):19-26. PubMed PMID: 12535855.