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| 50mg |
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Purity: ≥98%
Nebivolol (R065824; R-065824; Nobiten; Vasoxen) is a potent and selective beta1/β1-adrenoceptor antagonist with antihypertensive effects. It suppresses the β1-adrenoceptor with an IC50 of 0.8 nM. Nebivolol is a beta blocker that has been used to treat heart failure and high blood pressure.
| ln Vitro |
Nebivolol has antioxidative and potent stimulatory effects on endothelial nitric oxide synthase activity, which improve endothelial dysfunction[1].
Nebivolol (0.1 μM–10 μM, 1, 2, 4, 7 or 14 days) inhibits the proliferation of haCSMC or haEC, with IC50 values of approximately 6.0 μM[2]. Nebivolol (0.1 μM-10 μM, 24 h) causes apoptosis at a moderate rate[2]. Nebivolol (0.1, 1, 5, 10 μM, 4 days) causes HaCEs to secrete less endothelin-1 and to produce more NO[2]. |
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| ln Vivo |
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| Cell Assay |
Nebivolol (10-7~10-5 M) is added to human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) at varying concentrations for a period of 1, 2, 4, 7, and 14 days. Bromodeoxyuridine (BrdU) incorporation is used to analyze cell proliferation, while PI or annexin V staining is used to identify cell apoptosis.
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| Animal Protocol |
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| References |
| Molecular Formula |
C22H26CLF2NO4
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| Molecular Weight |
441.9
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| Exact Mass |
405.18
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| Elemental Analysis |
C, 65.17; H, 6.22; F, 9.37; N, 3.45; O, 15.78
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| CAS # |
118457-14-0
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| Related CAS # |
Nebivolol hydrochloride; 152520-56-4; (Rac)-Nebivolol; 99200-09-6; (rac)-Nebivolol-d4; 1219407-55-2
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| Appearance |
Solid powder
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| SMILES |
C1CC2=C(C=CC(=C2)F)O[C@H]1[C@H](CNC[C@@H]([C@@H]3CCC4=C(O3)C=CC(=C4)F)O)O
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| InChi Key |
KOHIRBRYDXPAMZ-YHDSQAASSA-N
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| 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/t17-,18-,21-,22+/m0/s1
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| Chemical Name |
(1S)-1-[(2S)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-[[(2S)-2-[(2R)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-hydroxyethyl]amino]ethanol
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2630 mL | 11.3148 mL | 22.6296 mL | |
| 5 mM | 0.4526 mL | 2.2630 mL | 4.5259 mL | |
| 10 mM | 0.2263 mL | 1.1315 mL | 2.2630 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05328310 | Active Recruiting |
Drug: Nebivolol | Hypertension | Korea University Anam Hospital | January 6, 2019 | Not Applicable |
| NCT05728632 | Active Recruiting |
Drug: Nebivolol Drug: Placebo |
Breast Cancer Cardiotoxicity |
Giulio Stefanini | January 1, 2019 | Phase 3 |
| NCT06104423 | Recruiting | Drug: Nebivolol 5 mg Drug: Ramipril 2.5/5/10 mg |
Hypertension | Menarini International Operations Luxembourg SA |
October 2, 2023 | Phase 4 |
| NCT06035978 | Not yet recruiting | Drug: Nebivolol Drug: Carvedilol |
Cardiovascular Diseases Heart Failure With Reduced Ejection Fraction |
University Hospital Ostrava | March 2024 | Phase 4 |
| NCT03778554 | Recruiting | Drug: Nebivolol Drug: Carvedilol Drug: Nebivolol |
Acute Myocardial Infarction ST Elevation Myocardial Infarction |
Bispebjerg Hospital | December 17, 2018 | Phase 4 |
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