Nebivolol hydrochloride

Modify Date: 2024-01-02 10:22:42

Nebivolol hydrochloride Structure
Nebivolol hydrochloride structure
Common Name Nebivolol hydrochloride
CAS Number 152520-56-4 Molecular Weight 441.896
Density N/A Boiling Point 600.5ºC at 760 mmHg
Molecular Formula C22H26ClF2NO4 Melting Point 220-222ºC
MSDS Chinese USA Flash Point 316.9ºC
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning

 Use of Nebivolol hydrochloride


Nebivolol hydrochloride selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.Target: β1- adrenergic receptorNebivolol 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.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.

 Names

Name Nebivolol Hydrochloride
Synonym More Synonyms

 Nebivolol hydrochloride Biological Activity

Description Nebivolol hydrochloride selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.Target: β1- adrenergic receptorNebivolol 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.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.
Related Catalog
References

[1]. Brehm BR, et al. Effects of nebivolol on proliferation and apoptosis of human coronary artery smooth muscle and endothelial cells. Cardiovasc Res. 2001 Feb 1;49(2):430-9.

[2]. Mercanoglu G, et al. The effects of nebivolol on apoptosis in a rat infarct model. Circ J. 2008 Apr;72(4):660-70.

 Chemical & Physical Properties

Boiling Point 600.5ºC at 760 mmHg
Melting Point 220-222ºC
Molecular Formula C22H26ClF2NO4
Molecular Weight 441.896
Flash Point 316.9ºC
Exact Mass 441.151855
PSA 70.95000
LogP 3.55650
Vapour Pressure 2.88E-15mmHg at 25°C
Storage condition Desiccate at RT
Water Solubility DMSO: ≥20mg/mL

 Safety Information

Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H302-H410
Precautionary Statements P273-P501
Hazard Codes Xn,N
Risk Phrases 22-50/53
Safety Phrases 60-61
RIDADR 3077
HS Code 2932999099

 Customs

HS Code 2932999099
Summary 2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles3

More Articles
Design, development and permeation studies of nebivolol hydrochloride from novel matrix type transdermal patches.

Adv. Biomed. Res. 2 , 62, (2013)

Nebivolol hydrochloride is a third generation β-blocker with highly selective β1-receptor antagonist with antihypertensive properties having plasma half life of 10 h and 12% oral bioavailability. The ...

Simultaneous estimation of amlodipine besylate and nebivolol hydrochloride in tablet dosage forms by reverse phase-high-performance liquid chromatographic using ultraviolet detection.

Pharm. Methods 2 , 9-14, (2013)

The present study aimed to develop and validate the simultaneous estimation of amlodipine and nebivolol in tablet dosage forms.An isocratic reversed phase high-performance liquid chromatographic (HPLC...

Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses.

FASEB J. 25 , 4486-97, (2011)

β-Adrenoceptor antagonists differ in their degree of partial agonism. In vitro assays have provided information on ligand affinity, selectivity, and intrinsic efficacy. However, the extent to which th...

 Synonyms

2H-1-Benzopyran-2-ethanaminium, 6-fluoro-N-[(2R)-2-[(2R)-6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl]-2-hydroxyethyl]-3,4-dihydro-β-hydroxy-, chloride, (βR,2S)- (1:1)
(S,R,R,R)-nebivolol hydrochloride
(2R)-2-[(2R)-6-Fluoro-3,4-dihydro-2H-chromen-2-yl]-N-{(2R)-2-[(2S)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-hydroxyethyl}-2-hydroxyethanaminium chloride
Nebivolol hydrochloride
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