| Size | Price | Stock | Qty |
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| 500mg |
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Purity: ≥98%
Marbofloxacin (Forcyl, Kelacyl, Zeniquin, Aristos, Boflox, Marbocyl, Aurizon), a carboxylic acid derivative, is a 3rd generation and broad spectrum antibiotic of the fluoroquinolone class used as a veterinary medication. Marbofloxacin showed notable antibacterial activity against both gram–and + bacteria.
| Targets |
Topoisomerase IV; Topoisomerase II
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| ln Vitro |
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| ln Vivo |
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| Animal Protocol |
SPF piglets inoculated intratracheally with M. hyopneumoniae strain 116
~2 mg/kg/day Intramuscular injection Tissue cages (TC), implanted subcutaneously in the neck in eight ponies, were inoculated with Staphylococcus aureus (S. aureus) to determine the clinical efficacy of marbofloxacin in the treatment of this infection. From 21 h after inoculation, marbofloxacin (6 mg/kg) was administered intravenously (i.v.) once daily for 7 days. Samples of the tissue cage fluid (TCF) were taken to determine marbofloxacin concentrations (days 1, 3 and 7), using high-pressure liquid chromatography, and numbers of viable bacteria [colony forming units (CFU)] (days 1, 3, 7, 14 and 21). Statistical analysis was used to compare CFU before and after treatment. Clinical signs and CFU were used to evaluate the efficacy of treatment. Although, there was a slight decrease in CFU in all TC initially, the infection was not eliminated by marbofloxacin treatment in any of the ponies and abscesses formed. As the MIC (0.25 microg/mL) did not change during treatment and the concentration of marbofloxacin during treatment (mean concentration in TCF was 0.89 microg/mL on day 1, 0.80 microg/mL on day 3 and 2.77 microg/mL on day 7) was above MIC, we consider that the treatment failure might be attributable to the formation of a biofilm by S. aureus. Based on the present results, i.v. administration of marbofloxacin alone is not suitable for the elimination of S. aureus infections from secluded sites.[2] |
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| ADME/Pharmacokinetics |
Marbofloxacin is a fluoroquinolone antibiotic expected to be effective in treating Gram-negative and some Gram-positive bacterial infections in horses. To develop a rational administration regimen for horses, this study conducted pharmacokinetic studies on six horses after intravenous, subcutaneous, and oral administration of a single dose of 2 mg/kg body weight of marbofloxacin, and determined its minimum inhibitory concentration (MIC) against bacteria isolated from equine pathogens. The mean clearance of marbofloxacin was 0.25 ± 0.05 L/kg/h, and the terminal half-life was 756 ± 1.99 h. The absolute bioavailability of marbofloxacin after subcutaneous and oral administration was 98 ± 11% and 62 ± 8%, respectively. The minimum inhibitory concentration (MIC90) required to inhibit 90% of the isolates was 0.027 μg/ml against Enterobacteriaceae and 0.21 μg/ml against Staphylococcus aureus. The surrogate endpoints for antimicrobial efficacy (AUIC, Cmax/MIC ratio, time above MIC90) were calculated, and the concentration curves of marbofloxacin after repeated dosing were simulated. These data were used to determine the appropriate dosing regimen for the target bacteria. Considering the breakpoint values of efficacy endpoints for fluoroquinolones, a marbofloxacin dosing regimen of 2 mg/kg body weight/24 h (intravenous, subcutaneous, or oral) was more appropriate for Enterobacteriaceae than for Staphylococcus aureus. [3]
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| Toxicity/Toxicokinetics |
US Patent No. 4801584: Oral LD50 in mice >2 g/kg
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| References | ||
| Additional Infomation |
LSM-5799 belongs to the quinoline class of compounds.
Marbofloxacin is a carboxylic acid and belongs to the third-generation antibiotic class of fluoroquinolones. It is used in veterinary medicine. Marbofloxacin is marketed as a combination of clotrimazole and dexamethasone under the brand name Aurizon. In the title compound [systematic name: 9-fluoro-2,3-dihydro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-7H-pyrido[1,2,3-ij][1,2,4]benzoxadiazine-6-carboxylic acid], C(17)H(19)FN(4)O(4), the carbonyl and carboxyl groups are coplanar with the quinoline ring, with a dihedral angle of 2.39 (2)°. The piperazine ring is in a chair conformation, and the oxadiazine ring is in an envelope conformation, with the CH(2) group at the ring opening deviating 0.650 (2) Å from the plane passing through the other five atoms. Due to the presence of intramolecular OH⋯O hydrogen bonds, the molecular structure exhibits an S(6) ring structure. In the crystal, weak CH⋯F hydrogen bonds connect the molecules into a layered structure parallel to the ab plane. [1] |
| Molecular Formula |
C17H19FN4O4
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| Molecular Weight |
362.36
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| Exact Mass |
362.139
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| Elemental Analysis |
C, 56.35; H, 5.29; F, 5.24; N, 15.46; O, 17.66
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| CAS # |
115550-35-1
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| Related CAS # |
115551-26-3
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| PubChem CID |
60651
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
570.5±60.0 °C at 760 mmHg
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| Melting Point |
268-269ºC
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| Flash Point |
298.8±32.9 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.701
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| LogP |
-0.55
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
636
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C([H])=C2C(C(C(=O)O[H])=C([H])N3C2=C(C=1N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])OC([H])([H])N3C([H])([H])[H])=O
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| InChi Key |
BPFYOAJNDMUVBL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H19FN4O4/c1-19-3-5-21(6-4-19)14-12(18)7-10-13-16(14)26-9-20(2)22(13)8-11(15(10)23)17(24)25/h7-8H,3-6,9H2,1-2H3,(H,24,25)
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| Chemical Name |
7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1,2-diazatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7597 mL | 13.7984 mL | 27.5969 mL | |
| 5 mM | 0.5519 mL | 2.7597 mL | 5.5194 mL | |
| 10 mM | 0.2760 mL | 1.3798 mL | 2.7597 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.
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.
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