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

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

MedKoo CAT#: 574810

CAS#: 99200-09-6

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

Chemical Structure

Nebivolol

CAS# 99200-09-6

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 574810
Name: Nebivolol
CAS#: 99200-09-6
Chemical Formula: C22H25F2NO4
Exact Mass: 405.18
Molecular Weight: 405.442
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	2 Weeks
25mg	USD 665	2 Weeks
100mg	USD 1125	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

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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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	100.0	246.64

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:	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.
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.

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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.

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