Nebivolol | CAS# 99200-09-6 | Cardioselective beta-1 receptor blocker

MedKoo Cat#: 574810 | Name: Nebivolol

Featured

Description:

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

Nebivolol is a cardioselective beta-1 receptor blocking agent and anti-hypertensive.

Chemical Structure

Nebivolol

CAS#99200-09-6

Theoretical Analysis

MedKoo Cat#: 574810

Name: Nebivolol

CAS#: 99200-09-6

Chemical Formula: C22H25F2NO4

Exact Mass: 405.1752

Molecular Weight: 405.44

Elemental Analysis: C, 65.17; H, 6.22; F, 9.37; N, 3.45; O, 15.78

Price and Availability

Size	Price	Availability
10mg	USD 340.00	2 Weeks
25mg	USD 665.00	2 Weeks
100mg	USD 1,125.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

Nebivolol

IUPAC/Chemical Name

α,α'-[Iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol]

InChi Key

KOHIRBRYDXPAMZ-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H25F2NO4/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

SMILES Code

OC(CNCC(C1CCC2=CC(F)=CC=C2O1)O)C3CCC4=CC(F)=CC=C4O3

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

>3 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 is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM.

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
	DMSO	100.0	246.64

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 405.44 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. Fongemie J, Felix-Getzik E. A Review of Nebivolol Pharmacology and Clinical Evidence. Drugs. 2015 Aug;75(12):1349-71. doi: 10.1007/s40265-015-0435-5. PMID: 26177892; PMCID: PMC4541699. 2. Battise D, Boland CL, Nuzum DS. Nebivolol/Valsartan: A Novel Antihypertensive Fixed-Dose Combination Tablet. Ann Pharmacother. 2019 Apr;53(4):402-412. doi: 10.1177/1060028018813575. Epub 2018 Nov 18. PMID: 30449127.