MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
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
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 Quantity
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 comments
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.

Recalculate based on batch purity %
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.
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.

View History

FNDP

FNDP