Levofloxacin

Synonyms: Fluoroquinolone

Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.

Levofloxacin Chemical Structure

Levofloxacin Chemical Structure

CAS No. 100986-85-4

Purity & Quality Control

Levofloxacin Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells Function assay 1.5 mins Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50=17.9 μM 23241029
human 5637 cells Function assay 200 to 300 ug/ml 12 h Antibacterial activity against uropathogenic Escherichia coli UTI89 infected in human 5637 cells assessed as decrease in intracellular bacterial level at 200 to 300 ug/ml after 12 hrs by serial dilution method 20231390
Click to View More Cell Line Experimental Data

Biological Activity

Description Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.
Targets
Topoisomerase II [1] Topoisomerase IV [1]
In vitro
In vitro Levofloxacin is active against most aerobic Gram-positive and Gram-negative organisms and demonstrates moderate activity against anaerobes.[1] Levofloxacin is two-fold more active than ciprofloxacin against Streptococcus pneumoniae and 2- to 4-fold more active than ciprofloxacin against Staphylococcus aureus, Xanthomonas maltophilia, and Bacteroides fragilis. Levofloxacin is two- to eightfold more active than ciprofloxacin against coagulase-negative staphylococci and Acinetobacter spp., although these improvements in potency may not be clinically relevant. Levofloxacin inhibits 90% of streptococci when it is used at concentrations of 1 mg/mL to 2 mg/mL. [2] Levofloxacin exhibits twofold greater inhibitory and bactericidal activities than ofloxacin against either extracellular or intracellular tubercle bacilli. [3] Levofloxacin has the least inhibitory effect on osteoblastic cell growth, with a 50% inhibitory concentration of approximately 80 mg/mL at 48 and 72 hours. Levofloxacin results in strong inhibition of calcium deposition, as determined on day 14 by alizarin red staining and biochemical analysis.[4] Levofloxacin inhibits glycosaminoglycan synthesis initially and DNA synthesis and mitochondrial function secondarily at actual arthropathic concentrations in cultured rabbit chondrocytes but that these changes are reversible and not enough to kill the cells. [5]
In Vivo
In vivo Levofloxacin is as efficacious as or more efficacious than that with ciprofloxacin in systemic as well as pyelonephritis infections in mice. Levofloxacin achieves higher concentrations in the serum and tissue of mice than does ciprofloxacin. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05743101 Not yet recruiting
Acute Ischemic Stroke
Yi Yang|The First Hospital of Jilin University
April 1 2024 Not Applicable
NCT05799326 Recruiting
Acute Ischemic Stroke
Yi Yang|The First Hospital of Jilin University
June 30 2023 Not Applicable
NCT05741905 Recruiting
Acute Ischemic Stroke
Yi Yang|The First Hospital of Jilin University
June 1 2023 Not Applicable
NCT05441930 Withdrawn
Cataract
PolyActiva Pty Ltd
June 23 2023 Phase 1

Chemical Information & Solubility

Molecular Weight 361.37 Formula

C18H20FN3O4

CAS No. 100986-85-4 SDF Download Levofloxacin SDF
Smiles CC1COC2=C3N1C=C(C(=O)C3=CC(=C2N4CCN(CC4)C)F)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 18 mg/mL ( (49.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 18 mg/mL

Ethanol : 2 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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