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Moxifloxacin HCl (BAY12-8039)

Alias: BAY12-8039 HCl; BAY-12-8039; BAY128039; Moxifloxacin hydrochloride; 186826-86-8; Moxifloxacin HCl; Avelox; Vigamox; Avalox; BAY 12-8039; Moxifloxacin (Hydrochloride); 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)
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.
Size Price Stock Qty
50mg
100mg
250mg
500mg
1g
2g
5g
Other Sizes

Other Forms of Moxifloxacin HCl (BAY12-8039):

  • Moxifloxacin (BAY12-8039)
  • Moxifloxacin hydrochloride monohydrate (BAY 12-8039 monohydrate)
  • (Rac)-Moxifloxacin ((Rac)-BAY 12-8039 free base)
  • Moxifloxacin-d4 (BAY 12-8039-d4 free base)
  • Moxifloxacin-d3 hydrochloride (BAY 12-8039-d3)
  • Moxifloxacin-d3-1 hydrochloride (moxifloxacin hydrochloride-d3; BAY 12-8039-d3-1)
  • rac cis-Moxifloxacin-d4 hydrochloride (rac cis-BAY 12-8039-d4)
Official Supplier of:
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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
In order to investigate the effect of moxifloxacin on survival, lipid peroxidation and inflammation in immunosuppressed rats with soft tissue infection caused by Stenotrophomonas maltophilia, 144 white male Wistar rats were randomized into six groups: Groups A and B received saline or moxifloxacin once per day, respectively; Groups C and D received saline or moxifloxacin twice per day, respectively, and Groups E and F received saline or moxifloxacin three times per day, respectively. Blood samples were taken at 6 and 30 hr after administration of S. maltophilia. Malonodialdehyde (MDA), WBC counts, bacterial tissue overgrowth, serum concentrations of moxifloxacin and survival were assessed. Survival analysis proved that treatment with moxifloxacin every 8 hr was accompanied by longer survival than occurred in any other group. Tissue cultures 30 hr after bacterial challenge showed considerably less bacterial overgrowth in the spleens and lungs of moxifloxacin-treated than in saline-treated animals, but not in their livers. At 6 hr there were no statistically significant differences between groups. However, at 30 hr, MDA concentrations were significantly greater (P = 0.044) and WBC counts significantly lower (P = 0.026) in group D than in group C. No statistically significant variations were observed between the other groups. Moxifloxacin possibly stimulates lipid peroxidation and enhances phagocytosis, as indicated by MDA production and survival prolongation, without being toxic, as indicated by WBC count. Therefore, under the appropriate conditions, moxifloxacin has a place in treatment of infections in immunosuppressed patients and of infections caused by S. maltophilia.[2]
Toxicity/Toxicokinetics
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the use of moxifloxacin during breastfeeding. Fluoroquinolones have traditionally not been used in infants because of concern about adverse effects on the infants' developing joints. However, recent studies indicate little risk. The calcium in milk might prevent absorption of the small amounts of fluoroquinolones in milk, but insufficient data exist to prove or disprove this assertion. Use of moxifloxacin is acceptable in nursing mothers with monitoring of the infant for possible effects on the gastrointestinal flora, such as diarrhea or candidiasis (thrush, diaper rash). However, it is preferable to use an alternate drug for which safety information is available.
Maternal use of an eye drop that contains moxifloxacin presents negligible risk for the nursing infant. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.
References

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

[2]. Microbiol Immunol. 2014 Feb;58(2):96-102.

Additional Infomation
Moxifloxacin hydrochloride is a hydrochloride comprising equimolar amounts of moxifloxacin and hydrogen chloride. It has a role as an antibacterial drug. It contains a moxifloxacinium(1+).
Moxifloxacin hydrochloride is an antibacterial prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment of certain bacterial infections, such as community-acquired pneumonia, acute worsening of chronic bronchitis, acute sinus infections, plague, and skin and abdominal infections.
Community-acquired pneumonia, a bacterial respiratory infection, can be an opportunistic infection (OI) of HIV.
Moxifloxacin Hydrochloride is the hydrochloride salt of a fluoroquinolone antibacterial antibiotic. Moxifloxacin binds to and inhibits the bacterial enzymes DNA gyrase (topoisomerase II) and topoisomerase IV, resulting in inhibition of DNA replication and repair and cell death in sensitive bacterial species.
A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.
See also: Moxifloxacin (has active moiety).
Drug Indication
Acute Exacerbation of Chronic Bronchitis, Community Acquired Pneumonia, Complicated Intra-Abdominal Infection, Complicated Skin and Skin Structure Infections, Pelvic Inflammatory Disease, Treatment of acute bacterial sinusitis
Acute Exacerbation of Chronic Bronchitis, Community Acquired Pneumonia, Complicated Intra-Abdominal Infection, Complicated Skin and Skin Structure Infections, Pelvic Inflammatory Disease, Treatment of acute bacterial sinusitis
Acute Exacerbation of Chronic Bronchitis, Community Acquired Pneumonia, Complicated Intra-Abdominal Infection, Complicated Skin and Skin Structure Infections, Pelvic Inflammatory Disease, Treatment of acute bacterial sinusitis
Acute Exacerbation of Chronic Bronchitis, Community Acquired Pneumonia, Complicated Intra-Abdominal Infection, Complicated Skin and Skin Structure Infections, Pelvic Inflammatory Disease, Treatment of acute bacterial sinusitis
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
437.151
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; Moxifloxacin Hydrochloride;186826-86-8;(Rac)-Moxifloxacin;354812-41-2;Moxifloxacin-d4;2596386-23-9;Moxifloxacin-d3 hydrochloride;2734919-98-1;Moxifloxacin-d3-1 hydrochloride;1246816-75-0;Moxifloxacin-13C,d3 hydrochloride;rac cis-Moxifloxacin-d4 hydrochloride;1217802-65-7
PubChem CID
101526
Appearance
Light yellow to green yellow solid powder
Boiling Point
636.4ºC at 760 mmHg
Flash Point
338.7ºC
Vapour Pressure
4.56E-17mmHg at 25°C
LogP
3.566
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
4
Heavy Atom Count
30
Complexity
727
Defined Atom Stereocenter Count
2
SMILES
Cl[H].FC1C([H])=C2C(C(C(=O)O[H])=C([H])N(C2=C(C=1N1C([H])([H])[C@]2([H])[C@@]([H])(C([H])([H])C([H])([H])C([H])([H])N2[H])C1([H])[H])OC([H])([H])[H])C1([H])C([H])([H])C1([H])[H])=O
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; Moxifloxacin hydrochloride; 186826-86-8; Moxifloxacin HCl; Avelox; Vigamox; Avalox; BAY 12-8039; Moxifloxacin (Hydrochloride); 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

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
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)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30mg/mL


Solubility in Formulation 4: 4 mg/mL (9.13 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C).

 (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

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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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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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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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