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Levofloxacin Topoisomerase inhibitor

Cat.No.S1940

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

Batch: Purity: 99.91%
99.91

Cell Culture, Treatment & Working Concentration

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
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
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Solubility

In vitro
Batch:

DMSO : 18 mg/mL (49.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 18 mg/mL

Ethanol : 2 mg/mL

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%
% Tween 80
% ddH2O
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Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight 361.37 Formula

C18H20FN3O4

Storage (From the date of receipt)
CAS No. 100986-85-4 Download SDF Storage of Stock Solutions

Synonyms Fluoroquinolone SMILES CC1COC2=C3N1C=C(C(=O)C3=CC(=C2N4CCN(CC4)C)F)C(=O)O

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
Topoisomerase II
Topoisomerase IV
In vitro
Levofloxacin is active against most aerobic Gram-positive and Gram-negative organisms and demonstrates moderate activity against anaerobes. This compound 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. It 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. This agent inhibits 90% of streptococci when it is used at concentrations of 1 mg/mL to 2 mg/mL. It exhibits twofold greater inhibitory and bactericidal activities than ofloxacin against either extracellular or intracellular tubercle bacilli.  This compound has the least inhibitory effect on osteoblastic cell growth, with a 50% inhibitory concentration of approximately 80 mg/mL at 48 and 72 hours. It results in strong inhibition of calcium deposition, as determined on day 14 by alizarin red staining and biochemical analysis. It 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.
In vivo
Levofloxacin is as efficacious as or more efficacious than that with ciprofloxacin in systemic as well as pyelonephritis infections in mice. This compound achieves higher concentrations in the serum and tissue of mice than does ciprofloxacin.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11117292/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8540702/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-30)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07675954 NOT_YET_RECRUITING
Rifampicin-Resistant Tuberculosis
Seoul National University Hospital
2026-10-01 PHASE3
NCT06810583 RECRUITING
Leukemia; Acute Myeloid Leukemia; Lymphoblastic Leukemia in Children
St. Jude Children's Research Hospital
2025-05-22 PHASE1
NCT07585461 NOT_YET_RECRUITING
Opportunistic Infections, HIV Related; Disseminated Mycobacterium Avium Complex Infection
Shanghai Public Health Clinical Center
2026-04-30
NCT07788404 RECRUITING
Prosthetic Joint Infection; Osteomyelitis; Staphylococcal Infections
Groupe Hospitalier Diaconesses Croix Saint-Simon
2023-06-10
NCT06494072 RECRUITING
Community Acquired Pneumonia in Children
Medical College of Wisconsin
2024-08-22 PHASE4
NCT07528417 NOT_YET_RECRUITING
Myeldysplastic Syndrome (MDS); MYELOPROLIFERATIVE DISORDER (P Vera, CMML, ET); Acute Myeloid Leukemia
University of Manitoba
2026-09-01 PHASE2

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