| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Nebivolol (also known as R-65824) potently and selectively inhibits β1-adrenoceptor with IC50 of 0.8 NM. Nebivolol demonstrates high selectivity and affinity for beta 1-adrenergic receptor sites in a lung membrane preparation from a rabbit (beta 2/beta 1 ratio = 50 and Ki value = 0.9 nM). With a Ki(β2)/Ki(β1) value of 40.7, which competition experiments judge to be 3H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, Kiβ2) or ICI 118.551 (50 nM, Kiβ1), Nebivolol exhibits β1-adrenoceptor selectivity.
| Targets |
β1-adrenoceptor ( IC50 = 0.8 nM )
|
|---|---|
| ln Vitro |
Nebivolol demonstrates high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (Ki value = 0.9 nM and beta 2/beta 1 ratio = 50).[1] Nebivolol demonstrates selectivity for β1-adrenoceptors with a Ki(β2)/Ki(β1) value of 40.7, as determined by competition experiments to 3H-CGP 12.1777 when CGP 207.12 A (300 nM, Kiβ2) or ICI 118.551 (50 nM, Kiβ1) are present.[2] Nebivolol inhibits human endothelial cells (haECs) and coronary smooth muscle cells (haCSMCs) in a manner that is concentration- and time-dependent. After 7 days of treatment, a significant reduction in the cell growth of haCSMCs is observed with an IC50 of 6.1 μM. Additionally, the accelerated proliferation of haCSMCs stimulated by growth factors TGFβ, bFGF, and PDGF-BB is inhibited with IC50 values of 6.8 μM, 6.4 μM, and 7.7 μM, respectively. After giving haCSMCs a 10-to 5-microgram dose of nibevolol for 48 hours, 23% of the cells undergo moderate apoptosis, and the proportion of S-phase cells falls from 16% to 5%. HaCEs produce more NO during Nebivolol incubation, but endothelin-1 transcription and secretion are inhibited.[3]
|
| ln Vivo |
Nebivolol administration reduces myocardial apoptosis in rats with myocardial infarction (MI). This effect is mediated by regulation of NO and occurs first by intravenous injection within 10 minutes of reperfusion and then orally. Nebivolol decreases both total and localized apoptotic cardiomyocytes and considerably prevents variations in left ventricular (LV) pressure. Treatment with nevivolol slightly but not significantly lowers the mean blood pressure (MBP) in rats suffering from MI.[4]
|
| Cell Assay |
Nebivolol (10-7~10-5 M) is added to cells at varying concentrations for 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.
|
| Animal Protocol |
Male Sprague Dawley rat myocardial infarction (MI) model
2.0 mg/kg Gastric gavage once daily |
| References | |
| Additional Infomation |
(S,R,R,R)-nebivolol hydrochloride is a hydrochloride obtained by reaction of (S,R,R,R)-nebivolol with one equivalent of hydrochloric acid. It contains a (S,R,R,R)-nebivolol(1+). It is an enantiomer of a (R,S,S,S)-nebivolol hydrochloride.
A cardioselective ADRENERGIC BETA-1 RECEPTOR ANTAGONIST (beta-blocker) that functions as a VASODILATOR through the endothelial L-arginine/ NITRIC OXIDE system. It is used to manage HYPERTENSION and chronic HEART FAILURE in elderly patients. See also: Nebivolol (has active moiety); Nebivolol hydrochloride; valsartan (component of). |
| Molecular Formula |
C22H26CLF2NO4
|
|---|---|
| Molecular Weight |
441.8960
|
| Exact Mass |
441.151
|
| Elemental Analysis |
C, 59.80; H, 5.93; Cl, 8.02; F, 8.60; N, 3.17; O, 14.48
|
| CAS # |
152520-56-4
|
| Related CAS # |
Nebivolol; 118457-14-0
|
| PubChem CID |
24866733
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
600.5ºC at 760 mmHg
|
| Melting Point |
220-222ºC
|
| Flash Point |
316.9ºC
|
| Vapour Pressure |
2.88E-15mmHg at 25°C
|
| LogP |
3.556
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
30
|
| Complexity |
483
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
Cl[H].FC1C([H])=C([H])C2=C(C=1[H])C([H])([H])C([H])([H])[C@]([H])(C([H])(C([H])([H])N([H])C([H])([H])[C@@]([H])([C@]1([H])C([H])([H])C([H])([H])C3C([H])=C(C([H])=C([H])C=3O1)F)O[H])O[H])O2
|
| InChi Key |
JWEXHQAEWHKGCW-BIISKSHESA-N
|
| InChi Code |
InChI=1S/C22H25F2NO4.ClH/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;1H/t17-,18-,21-,22+;/m0./s1
|
| 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;hydrochloride
|
| Synonyms |
Silostar; Bystolic; R 67145; R-67145; R67145; Nebivolol HCl; Nebivolol Hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 88~100 mg/mL (199.1~226.3 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO + 20% PEG300 + 5%Tween 80 + 70%ddH2O: 4.4mg/ml (9.96mM) |
| 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 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
