Home DNA Damage/DNA Repair Topoisomerase inhibitor Moxifloxacin (BAY12-8039) HCl For research use only.

Moxifloxacin (BAY12-8039) HCl

Synonyms: Avelox, Avalox,BAY12-8039 HCl

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

Moxifloxacin (BAY12-8039) HCl Chemical Structure

Moxifloxacin (BAY12-8039) HCl Chemical Structure

CAS: 186826-86-8

Selleck's Moxifloxacin (BAY12-8039) HCl has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.87%
99.87

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Biological Activity

Description Moxifloxacin (Avelox, Avalox,BAY12-8039 HCl) is a fourth-generation synthetic fluoroquinolone antibacterial agent.
Targets
Topoisomerase II [1] Topoisomerase IV [1]
In vitro
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. [1]
In Vivo
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. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06107036 Not yet recruiting Healthy Boehringer Ingelheim February 26 2024 Phase 1
NCT05893862 Recruiting Schizophrenia Merck Sharp & Dohme LLC June 26 2023 Phase 1
NCT05878522 Active not recruiting Healthy Pfizer May 15 2023 Phase 1

Chemical lnformation & Solubility

Molecular Weight 437.89 Formula

C21H24FN3O4.HCl
CAS No. 186826-86-8 SDF Download Moxifloxacin (BAY12-8039) HCl SDF
Smiles COC1=C2C(=CC(=C1N3CC4CCCNC4C3)F)C(=O)C(=CN2C5CC5)C(=O)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (200.96 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh 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.

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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