Moxifloxacin HCl (BAY12-8039)

Alias: BAY12-8039 HCl; BAY-12-8039; BAY128039; BAY-128039; BAY 128039; Moxifloxacin; BAY12-8039; BAY 12-8039; Avelox; Avalox; Avelon; Vigamox; Moxeza
Cat No.:V1416 Purity: ≥98%
Moxifloxacin HCl (formerly BAY12-8039; BAY12-8039; BAY 12-8039; Avelox; Avalox; Avelon; Vigamox; Moxeza), the hydrochloride salt of moxifloxacin, is an orally bioactive, broad spectrum and 4th generation antibacterial drug of the fluoroquinolone class with high activity against both Gram positive and Gram negative bacteria.
Moxifloxacin HCl (BAY12-8039) Chemical Structure CAS No.: 186826-86-8
Product category: Topoisomerase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Moxifloxacin HCl (formerly BAY12-8039; BAY12-8039; BAY 12-8039; Avelox, Avalox, Avelon, Vigamox, Moxeza),the hydrochloride salt of moxifloxacin, is an orally bioactive, broad spectrum and 4th generation antibacterial drug of the fluoroquinolone class with high activity against both Gram positive and Gram negative bacteria. It functions as a topoisomerase II and IV DNA inhibitor.

Biological Activity I Assay Protocols (From Reference)
Targets
Topoisomerase II; Topoisomerase IV
ln Vitro

In vitro activity: Moxifloxacin has an action that involves entangling a DNA drug enzyme complex and specifically blocking the ATP-dependent enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. Moxipovexacin exhibits a minimum inhibitory concentration (MIC) of 0.177 μg/mL in vitro against M. tuberculosis H37Rv. Both Grampositive and Gramnegative activity are widely distributed in methyloxacin. Antibiotics such as Staphylococcus aureus, Streptococcus pneumoniae, Streptopyogenes, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Chlamydia pneumoniae, and Mycoplasma pneumoniae are all effectively combatted by moxiloxacin in vitro and cliniquely. 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 is 16 μg/mL for M. chelonae and 0.5 μg/mL for M. fortuitum.[1]

ln Vivo
Moxifloxacin combined with RIF/pyrazinamide (PZA) in a mouse model intended to mimic human disease shortens treatment duration by up to two months when compared to regimens with isoniazid (INH)/RIF/PZA. Mice treated twice weekly with RIF/Moxifloxacin/PZA show similar results, reaching a stable cure after 4 months, while daily treatment with RIF/INH/PZA results in a cure in 6 months. In mice, 100 mg/kg of Moxipovoxacin produces activity equivalent to that of INH; a daily dose of 400 mg/kg of Moxipovoxacin causes spleen CFU counts to be lower than those of INH, which are 25 mg/kg, but the differences are not statistically significant. In a mouse model of tuberculosis, the AUC/MIC ratio most closely corresponds with the in-vivo efficacy of fluoroquinolones. [1]
Cell Assay
The antibiotic agent doxifloxacin (hydrochloride) is a synthetic fluoroquinolone. When compared to earlier fluoroquinolone agents, antibacterial doxifloxacin, an extended-spectrum fluoroquinolone, exhibits better coverage against gram-positive cocci and atypical pathogens while maintaining good activity against gram-negative bacteria. All common upper and lower respiratory tract pathogens are included in moxifloxacin's antibacterial spectrum, making it one of the most effective fluoroquinolones against pneumococci, including strains resistant to macrolides and penicillin. Moxifloxacin's potential for phototoxicity is limited. Moxifloxacin demonstrated bacteriologic eradication rates of 90–97% and clinical success rates of 88–97% in clinical trials. Moxifloxacin is an antimicrobial agent that is both safe and effective in treating community-acquired pneumonia, acute bacterial exacerbations of chronic bronchitis, and acute sinusitis. As shown by the production of MDA and the prolongation of survival, movifloxacin may promote lipid peroxidation and improve phagocytosis without being toxic, as shown by the white blood cell count. Clinical recommendations: Acute sinusitis, bacterial infection, acute bronchitis, and abdominal abscess toxicity CNS and gastrointestinal side effects, such as reduced activity, sleepiness, trembling, convulsions, vomiting, and diarrhea, are signs of an overdose. In rats and mice, a minimal lethal intravenous dose is 100 mg/kg.
Animal Protocol
144 white male Wistar rats (18-22 weeks; 300-400 g) infected Stenotrophomonas maltophilia
12 mg/kg
Intravenous injection; once per day, twice per day, three times per day; for 7 days
References

[1]. Tuberculosis (Edinb) . 2008 Mar;88(2):127-31.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H24FN3O4.HCL
Molecular Weight
437.89
Exact Mass
437.15
Elemental Analysis
C, 57.60; H, 5.75; Cl, 8.10; F, 4.34; N, 9.60; O, 14.61
CAS #
186826-86-8
Related CAS #
151096-09-2;192927-63-2
Appearance
Solid powder
SMILES
COC1=C2C(=CC(=C1N3C[C@@H]4CCCN[C@@H]4C3)F)C(=O)C(=CN2C5CC5)C(=O)O.Cl
InChi Key
IDIIJJHBXUESQI-DFIJPDEKSA-N
InChi Code
InChI=1S/C21H24FN3O4.ClH/c1-29-20-17-13(19(26)14(21(27)28)9-25(17)12-4-5-12)7-15(22)18(20)24-8-11-3-2-6-23-16(11)10-24;/h7,9,11-12,16,23H,2-6,8,10H2,1H3,(H,27,28);1H/t11-,16+;/m0./s1
Chemical Name
7-[(4aS,7aS)-1,2,3,4,4a,5,7,7a-octahydropyrrolo[3,4-b]pyridin-6-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxoquinoline-3-carboxylic acid;hydrochloride
Synonyms
BAY12-8039 HCl; BAY-12-8039; BAY128039; BAY-128039; BAY 128039; Moxifloxacin; BAY12-8039; BAY 12-8039; Avelox; Avalox; Avelon; Vigamox; Moxeza
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 25~88 mg/mL (57.1~201 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
30% PEG400+0.5% Tween80+5%Propylene glycol: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2837 mL 11.4184 mL 22.8368 mL
5 mM 0.4567 mL 2.2837 mL 4.5674 mL
10 mM 0.2284 mL 1.1418 mL 2.2837 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

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

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05660720 Active
Recruiting
Drug: Orelabrutinib and placebo
(orelabrutinib tablet simulator)
Drug: Orelabrutinib
Healthy Subject Beijing InnoCare Pharma Tech
Co., Ltd.
November 19, 2022 Phase 1
NCT05924815 Active
Recruiting
Drug: Aficamten
Drug: Moxifloxacin
Healthy Participants Cytokinetics May 15, 2023 Phase 1
NCT03236961 Active
Recruiting
Drug: Ertapenem
Drug: Moxifloxacin
Acute Appendicitis Turku University Hospital April 3, 2017 Not Applicable
NCT05878522 Active
Recruiting
Drug: moxifloxacin
Drug: placebo
Healthy Pfizer May 15, 2023 Phase 1
NCT04179500 Active
Recruiting
Drug: moxifloxacin
Drug: pyrazinamide
Tuberculosis, MDR
Tuberculosis
Global Alliance for TB Drug
Development
September 16, 2021 Phase 2
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