Moxifloxacin

Fluoroquinolone antibiotic,board specturm CAS# 151096-09-2

Moxifloxacin

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Chemical structure

Moxifloxacin

3D structure

Chemical Properties of Moxifloxacin

Cas No. 151096-09-2 SDF Download SDF
PubChem ID 152946 Appearance Powder
Formula C21H24FN3O4 M.Wt 401.43
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
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
SMILES COC1=C2C(=CC(=C1N3CC4CCCNC4C3)F)C(=O)C(=CN2C5CC5)C(=O)O
Standard InChIKey FABPRXSRWADJSP-MEDUHNTESA-N
Standard InChI InChI=1S/C21H24FN3O4/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)/t11-,16+/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Moxifloxacin

DescriptionMoxifloxacin is a synthetic fluoroquinolone antibiotic agent. Target: Antibacterial Moxifloxacin is an extended-spectrum fluoroquinolone which has improved coverage against gram-positive cocci and atypical pathogens compared with older fluoroquinolone agents, while retaining good activity against gram-negative bacteria. The antibacterial spectrum of moxifloxacin includes all major upper and lower respiratory tract pathogens; it is one of the most active fluoroquinolones against pneumococci, including penicillin- and macrolide-resistant strains [1]. Moxifloxacin has limited phototoxic potential. In clinical trials, moxifloxacin had clinical success rates of 88-97% and bacteriologic eradication rates of 90-97%. Moxifloxacin is a safe and effective antimicrobial that will be useful for treating acute sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [2]. Moxifloxacin possibly stimulates lipid peroxidation and enhances phagocytosis, as depicted by MDA production and survival prolongation, without being toxic as depicted by white blood cell count [3]. Clinical indications: Abdominal abscess; Acute bronchitis; Acute sinusitis; Bacterial infection Toxicity: Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.

References:
[1]. Balfour, J.A. and H.M. Lamb, Moxifloxacin: a review of its clinical potential in the management of community-acquired respiratory tract infections. Drugs, 2000. 59(1): p. 115-39. [2]. Culley, C.M., et al., Moxifloxacin: clinical efficacy and safety. Am J Health Syst Pharm, 2001. 58(5): p. 379-88. [3]. Ioannidis, O., et al., Effect of moxifloxacin on the survival, lipid peroxidation and inflammation of immunosuppressed rats with soft tissue infection from Stenotrophomonas maltophilia. Microbiol Immunol, 2013.

Moxifloxacin Dilution Calculator

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Moxifloxacin Molarity Calculator

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Preparing Stock Solutions of Moxifloxacin

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4911 mL 12.4555 mL 24.9109 mL 49.8219 mL 62.2774 mL
5 mM 0.4982 mL 2.4911 mL 4.9822 mL 9.9644 mL 12.4555 mL
10 mM 0.2491 mL 1.2455 mL 2.4911 mL 4.9822 mL 6.2277 mL
50 mM 0.0498 mL 0.2491 mL 0.4982 mL 0.9964 mL 1.2455 mL
100 mM 0.0249 mL 0.1246 mL 0.2491 mL 0.4982 mL 0.6228 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Moxifloxacin

Moxifloxacin is an orally bio-available, broad spectrum bacterial gyrase-inhibiting fluoroquinolone antibiotic [1].

Moxifloxacin at 50 μg/mL has been reported to induce a significant reduction of viable cells. A remarkable anti-proliferative activity of moxifloxacin has been proved in the concentrations between 50 and 1500 μg/mL. Moreover, moxifloxacin could lead to signs of cellular damage which were seen like binucleation in a dose-dependent manner [2].

Rats intravenously injected with moxifloxacin at 100 mg/kg have shown the increase of Serum glucose and serum epinephrine concentrations as well as the release of histamine. However, moxifloxacin at 75 mg/kg did not show any effects on serum epinephrine, glucose or histamine concentrations increase [3].

References:
[1] Iatropoulos MJ1, Jeffrey AM, Enzmann HG, von Keutz E, Schlueter G, Williams GM. Assessment of chronic toxicity and carcinogenicity in an accelerated cancer bioassay in rats of moxifloxacin, a quinolone antibiotic. Exp Toxicol Pathol. 2001 Oct;53(5):345-57.
[2] Sobolewska B1, Hofmann J, Spitzer MS, Bartz-Schmidt KU, Szurman P, Yoeruek E. Antiproliferative and cytotoxic properties of moxifloxacin on rat retinal ganglion cells. Curr Eye Res. 2013 Jun;38(6):662-9.
[3] Ishiwata Y1, Takahashi Y, Nagata M, Yasuhara M. Effects of moxifloxacin on serum glucose concentrations in rats. Biol Pharm Bull. 2013;36(4):686-90.

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References on Moxifloxacin

Efficacy of Triple Antibiotic Paste, Moxifloxacin, Calcium Hydroxide And 2% Chlorhexidine Gel In Elimination of E. Faecalis: An In vitro Study.[Pubmed:28274034]

J Clin Diagn Res. 2017 Jan;11(1):ZC06-ZC09.

INTRODUCTION: Root canal treatment is incomplete without usage of intra canal medicaments. They help in the reduction of bacterial count and its by-products, making canals clean and decreasing postoperative pains. AIM: The aim of this study was to evaluate and compare the antimicrobial activity of triple antibiotic paste, Moxifloxacin, calcium hydroxide and 2% Chlorhexidine (CHX) gel in elimination of Enterococcous faecalis (E. faecalis). MATERIALS AND METHODS: Seventy-five root blocks were obtained from extracted single rooted human teeth. The canal diameter was increased using Gates- Glidden drill up to size 3 and then contaminated with E. faecalis for 21 days. The contaminated samples were then divided into following 5 groups. Group 1: Saline (negative group), Group 2: Calcium hydroxide Ca(OH)2, Group 3: 2% CHX gel, Group 4: Triple Antibiotic Paste (TAP) (50 mug - metronidazole of 400 mg, 50 mug - minocycline of 100 mg, 50 mug - ciprofloxacin of 100 mg) and Group 5: Moxifloxacin (50 mug - Moxifloxacin of 400 mg). Dentin debris was obtained at the end of first, 7(th), and 10(th) day using Gates Glidden drill sizes 4 and 5. The bacterial load was assessed by counting the number of Colony Forming Units (CFUs). The data were analyzed with the ANOVA and Post-Hoc tests to assess the differences in antibacterial efficacy between groups (p=<0.001). RESULTS: A 2% CHX gel alone completely inhibited the growth of E. faecalis after one, seven and 10 days. The 2% CHX gel was the most effective medicament against E. faecalis, as it showed significant differences with normal saline, calcium hydroxide, Moxifloxacin or triple antibiotic paste at all time intervals. The triple antibiotic paste group showed a moderate antibacterial effect as its difference with all group was significantly better at all days. Moxifloxacin was more effective than calcium hydroxide on 7(th) and 10(th) day. CONCLUSION: Best antimicrobial efficacy was shown by 2% CHX gel. Moxifloxacin was equally efficient compared to triple antibiotic paste against E. faecalis at longer intervals of time.

Description

Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.

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