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Tocris/Nebivolol hydrochloride/3517/10/10 mg

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货号: 3517/10

品牌: Tocris

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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 Technical Data Solubility Calculators Datasheets References

Biological Activity

Highly selective β₁-adrenoceptor antagonist (K_i values are 0.88, 20, 44, 700, 1160, 2400 and 4000 nM at β₁, 5-HT_1A, 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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

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

Keywords: Nebivolol hydrochloride, supplier, selective, α1-adrenoceptor, beta1-adrenoceptor, b1-adrenoceptor, b1-adrenergic, antagonists, β1-Adrenergic, beta1-Adrenergic, Receptors, Adrenergic, Beta-1, Receptors, Adrenergic, Beta-1, Receptors, Tocris Bioscience

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