Levonebivolol

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 319892

CAS#: 118457-16-2

Description: Levonebivolol, also known as R 67145, is an enantiomer of Nebivolol which is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and, in Europe, also for left ventricular failure. It is highly cardioselective under certain circumstances.

Chemical Structure

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Levonebivolol
CAS# 118457-16-2
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 319892
Name: Levonebivolol
CAS#: 118457-16-2
Chemical Formula: C22H25F2NO4
Exact Mass: 405.18
Molecular Weight: 405.442
Elemental Analysis: C, 65.17; H, 6.22; F, 9.37; N, 3.45; O, 15.78

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: R67145; R-67145; R 67145; Levonebivolol

IUPAC/Chemical Name: (S)-1-((R)-6-fluorochroman-2-yl)-2-(((S)-2-((S)-6-fluorochroman-2-yl)-2-hydroxyethyl)amino)ethan-1-ol

InChi Key: KOHIRBRYDXPAMZ-YHDSQAASSA-N

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

SMILES Code: O[C@@H](CNC[C@@H]([C@H]1CCC2=CC(F)=CC=C2O1)O)[C@@H]3CCC4=CC(F)=CC=C4O3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: Nebivolol (R 065824) is an orally active beta receptor blocker and has the high beta(1)-receptor affinity.
In vitro activity: Nebivolol inhibited accelerated haCSMC proliferation even in the presence of growth factors such as TGFbeta(1) and PDGF-BB. Nebivolol concentration-dependently induced a moderate apoptosis (10(-5) mol/l: 23%) and a decrease of haCSMCs in the S-phase by 66%. HaECs showed comparable results. Reference: Cardiovasc Res. 2001 Feb 1;49(2):430-9. https://pubmed.ncbi.nlm.nih.gov/11164853/
In vivo activity: Nebivolol treatment partially recovered glomerular filtration rate, improved renal injury, normalized blood pressure and attenuated renal vasoconstriction in Wistar rats. Reference: Front Med (Lausanne). 2022 Aug 4;9:953749. https://pubmed.ncbi.nlm.nih.gov/35991671/

Preparing Stock Solutions

The following data is based on the product molecular weight 405.44 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Bueno-Pereira TO, Nunes PR, Matheus MB, Vieira da Rocha AL, Sandrim VC. Nebivolol Increases Nitric Oxide Synthase via β3 Adrenergic Receptor in Endothelial Cells Following Exposure to Plasma from Preeclamptic Patients. Cells. 2022 Mar 4;11(5):883. doi: 10.3390/cells11050883. PMID: 35269505; PMCID: PMC8909669. 2. Brehm BR, Wolf SC, Bertsch D, Klaussner M, Wesselborg S, Schüler S, Schulze-Osthoff K. Effects of nebivolol on proliferation and apoptosis of human coronary artery smooth muscle and endothelial cells. Cardiovasc Res. 2001 Feb 1;49(2):430-9. doi: 10.1016/s0008-6363(00)00253-4. PMID: 11164853. 3. Nascimento MM, Bernardo DRD, de Bragança AC, Massola Shimizu MH, Seguro AC, Volpini RA, Canale D. Treatment with β-blocker nebivolol ameliorates oxidative stress and endothelial dysfunction in tenofovir-induced nephrotoxicity in rats. Front Med (Lausanne). 2022 Aug 4;9:953749. doi: 10.3389/fmed.2022.953749. PMID: 35991671; PMCID: PMC9386005. 4. Naeem AG, El-Naga RN, Michel HE. Nebivolol elicits a neuroprotective effect in the cuprizone model of multiple sclerosis in mice: emphasis on M1/M2 polarization and inhibition of NLRP3 inflammasome activation. Inflammopharmacology. 2022 Dec;30(6):2197-2209. doi: 10.1007/s10787-022-01045-4. Epub 2022 Aug 10. PMID: 35948811; PMCID: PMC9700639.
In vitro protocol: 1. Bueno-Pereira TO, Nunes PR, Matheus MB, Vieira da Rocha AL, Sandrim VC. Nebivolol Increases Nitric Oxide Synthase via β3 Adrenergic Receptor in Endothelial Cells Following Exposure to Plasma from Preeclamptic Patients. Cells. 2022 Mar 4;11(5):883. doi: 10.3390/cells11050883. PMID: 35269505; PMCID: PMC8909669. 2. Brehm BR, Wolf SC, Bertsch D, Klaussner M, Wesselborg S, Schüler S, Schulze-Osthoff K. Effects of nebivolol on proliferation and apoptosis of human coronary artery smooth muscle and endothelial cells. Cardiovasc Res. 2001 Feb 1;49(2):430-9. doi: 10.1016/s0008-6363(00)00253-4. PMID: 11164853.
In vivo protocol: 1. Nascimento MM, Bernardo DRD, de Bragança AC, Massola Shimizu MH, Seguro AC, Volpini RA, Canale D. Treatment with β-blocker nebivolol ameliorates oxidative stress and endothelial dysfunction in tenofovir-induced nephrotoxicity in rats. Front Med (Lausanne). 2022 Aug 4;9:953749. doi: 10.3389/fmed.2022.953749. PMID: 35991671; PMCID: PMC9386005. 2. Naeem AG, El-Naga RN, Michel HE. Nebivolol elicits a neuroprotective effect in the cuprizone model of multiple sclerosis in mice: emphasis on M1/M2 polarization and inhibition of NLRP3 inflammasome activation. Inflammopharmacology. 2022 Dec;30(6):2197-2209. doi: 10.1007/s10787-022-01045-4. Epub 2022 Aug 10. PMID: 35948811; PMCID: PMC9700639.

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