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Submit ReviewNebivolol hydrochloride
Description: Highly selective β1-adrenoceptor antagonist
Chemical Name: (±)-[2R*(1S*5S*(S*))]-α,α'-[Iminobis(methylene)bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol)
Purity: ≥98% (HPLC)
Biological Activity for Nebivolol hydrochloride
Nebivolol hydrochloride is a highly selective β1-adrenoceptor antagonist (Ki values are 0.88, 20, 44, 700, 1160, 2400 and 4000 nM at β1, 5-HT1A, β2, 5-HT2, α1, H1 and D2 receptors respectively). Induces vasodilation via a nitric oxide- and cGMP-dependent mechanism (EC50 = 11.36 μM in renal arteries) and displays antihypertensive activity in vivo. GRK/β -arrestin biased agonist at the β2 adrenoceptor.
Compound Libraries for Nebivolol hydrochloride
Nebivolol hydrochloride is also offered as part of the Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Nebivolol hydrochloride
| M. Wt | 441.9 |
| Formula | C22H25F2NO4.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 152520-56-4 |
| PubChem ID | 11812257 |
| InChI Key | JWEXHQAEWHKGCW-VCVZPGOSSA-N |
| Smiles | FC(C=C4)=CC3=C4O[C@@](CC3)([H])[C@H](O)CNC[C@@H](O)[C@]2([H])CCC1=CC(F)=CC=C1O2.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Nebivolol hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.19 | 100 | |
| ethanol | 4.42 | 10 |
Preparing Stock Solutions for Nebivolol hydrochloride
The following data is based on the product molecular weight 441.9. 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 | 2.26 mL | 11.31 mL | 22.63 mL |
| 5 mM | 0.45 mL | 2.26 mL | 4.53 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.26 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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Product Datasheets for Nebivolol hydrochloride
References for Nebivolol hydrochloride
References are publications that support the biological activity of the product.
Pauwels et al (1988) The receptor binding profile of the new antihypertensive agent nebi. and its stereoisomers compared with various β-adrenergic blockers. Mol.Pharmacol. 34 843 PMID: 2462161
Georgescu et al (2008) Nebivolol induces a hyperpolarizing effect on smooth muscle cells in the mouse renal artery by activation of beta-2-adrenoceptors. Pharmacology 81 110 PMID: 17952013
Erickson et al (2013) The beta -blocker nebi. Is a GRK/ beta -arrestin biased agonist. PLoS One 8 e71980 PMID: 23977191
If you know of a relevant reference for Nebivolol hydrochloride, please let us know.
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1 Citation for Nebivolol hydrochloride
Citations are publications that use Tocris products. Selected citations for Nebivolol hydrochloride include:
Littmann et al (2015) Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands. Brain Res 355 183 PMID: 26306764
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.