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Moxifloxacin (BAY12-8039) HCl Topoisomerase inhibitor

Cat.No.S1465

Moxifloxacin (Avelox, Avalox,BAY12-8039 HCl) is a fourth-generation synthetic fluoroquinolone antibacterial agent.
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Quality Control

Batch: Purity: 99.87%
99.87

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (200.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 18 mg/mL

Ethanol : Insoluble

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 437.89 Formula

C21H24FN3O4.HCl

Storage (From the date of receipt)
CAS No. 186826-86-8 Download SDF Storage of Stock Solutions

Synonyms Avelox, Avalox,BAY12-8039 HCl SMILES COC1=C2C(=CC(=C1N3CC4CCCNC4C3)F)C(=O)C(=CN2C5CC5)C(=O)O.Cl

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Mechanism of Action

Targets/IC50/Ki
Topoisomerase II
Topoisomerase IV
In vitro

Moxifloxacin exerts its effects by trapping a DNA drug enzyme complex and specifically inhibiting ATP-dependent enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. Moxifloxacin shows in-vitro potency against M. tuberculosis H37Rv with MIC of 0.177 μg/mL. Moxifloxacin has broad Grampositive and Gram-negative activity. Moxifloxacin shows in vitro and clinical efficacy against Staphylococcus aureus, Streptococcus pneumoniae, Str. pyogenes, Haemophilus influenzae, H. parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Chlamydia pneumoniae and Mycoplasma pneumoniae. Moxifloxacin has activity against mycobacteria in addition to M. tuberculosis; Moxifloxacin is more active against M. kansasii than M. avium complex: specifically MIC90 for M. avium > M. intracellulare > M. kansasii at 4, 2 and 2 μg/mL, respectively. MIC90 for M. chelonae > M. fortuitum at 16 and 0.5 μg/mL, respectively.

In vivo

Moxifloxacin combined with RIF/pyrazinamide (PZA) reduces treatment time by up to 2 months compared to regimens with isoniazid (INH)/RIF/PZA in a mouse model designed to mimic human disease. Similar results with a stable cure are reached after 4 months in mice treated twice weekly with RIF/Moxifloxacin/PZA compared to cure in 6 months when daily treated with RIF/INH/PZA. 100 mg/kg Moxifloxacin in mice gives activity comparable to INH; increased dose in mice to 400 mg/kg Moxifloxacin daily results in spleen CFU counts lower than for INH 25 mg/kg although the differences are not statistically significant. AUC/MIC ratio correlates best with in-vivo efficacy for the fluoroquinolones in a mouse model of tuberculosis.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-02)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06441006 RECRUITING
Tuberculosis, Pulmonary; Tuberculosis, Multidrug-Resistant; Tuberculosis, MDR
University of California, San Francisco
2025-10-03 PHASE2; PHASE3
NCT07485010 NOT_YET_RECRUITING
Mycobacterium Abscessus Pulmonary Disease; Mycobacterium Abscessus Infection; Non-Tuberculous Mycobacterial (NTM) Infections; Non-Tuberculous Mycobacteria Pulmonary Disease
The University of Queensland
2027-04 PHASE2
NCT03244072 NOT_YET_RECRUITING
Endophthalmitis
Jason Ahee, M.D.
2026-06-01 PHASE2; PHASE3
NCT04310930 RECRUITING
Pulmonary Disease Due to Mycobacteria (Diagnosis)
The University of Queensland
2020-03-02 PHASE2; PHASE3
NCT07595042 NOT_YET_RECRUITING
Tuberculosis
National Institute of Allergy and Infectious Diseases (NIAID)
2026-10-30 PHASE2
NCT07585461 NOT_YET_RECRUITING
Opportunistic Infections, HIV Related; Disseminated Mycobacterium Avium Complex Infection
Shanghai Public Health Clinical Center
2026-04-30

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