Biological Activity
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
Nebivolol hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
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.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 44.19 | 100 | |
ethanol | 4.42 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 441.9. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
Pauwels et al (1988) The receptor binding profile of the new antihypertensive agent nebivolol 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 Nebivolol Is a GRK/ beta -arrestin biased agonist. PLoS One 8 e71980 PMID: 23977191
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