| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Targets |
Bacterial DNA gyrase (topoisomerase II) and topoisomerase IV. Orbifloxacin is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase in Gram-negative bacteria and topoisomerase IV in Gram-positive bacteria. DNA gyrase is an essential enzyme that introduces negative supercoils into DNA, which is critical for DNA replication and transcription. Topoisomerase IV is involved in the decatenation of replicated DNA chromosomes. By inhibiting these enzymes, Orbifloxacin blocks DNA replication and transcription, leading to bacterial cell death. The compound is a synthetic fluoroquinolone antibacterial agent. Orbifloxacin exhibits in vitro activity against a wide range of Gram-positive and Gram-negative bacteria, enterobacteriaceae, anaerobes, and mycobacteria. The compound was developed as a veterinary chemotherapeutic.
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| ln Vitro |
Orbifloxacin demonstrates antibacterial activity in vitro against a wide range of Gram-positive and Gram-negative bacteria, enterobacteriaceae, anaerobes, and mycobacteria. Its antibacterial activity is assessed by standard antimicrobial susceptibility testing methods (broth microdilution or agar diffusion). The compound's minimum inhibitory concentrations (MICs) against various bacterial strains have been characterized. Like other fluoroquinolones, the bactericidal action of orbifloxacin results from inhibition of DNA gyrase and topoisomerase IV. Orbifloxacin was developed as a veterinary chemotherapeutic for livestock and domestic pets. The compound is a synthetic fluoroquinolone antibacterial agent.
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| ln Vivo |
Orbifloxacin is used in veterinary medicine for the treatment of bacterial infections in livestock and domestic pets. The compound's in vivo efficacy has been established through veterinary use. Orbifloxacin exhibits in vitro activity against a wide range of Gram-positive and Gram-negative bacteria, enterobacteriaceae, anaerobes, and mycobacteria. The compound is administered orally or by injection in veterinary practice. Detailed pharmacokinetic and pharmacodynamic data are available from veterinary studies. Orbifloxacin is for research use only and is not for human therapeutic use.
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| Enzyme Assay |
Antibacterial susceptibility testing is performed using broth microdilution or agar dilution methods according to CLSI guidelines. Bacterial strains (e.g., E. coli ATCC 25922, S. aureus ATCC 29213) are cultured in appropriate media (e.g., Mueller-Hinton broth or agar). Orbifloxacin is serially diluted in 96-well plates or agar plates. Bacterial inoculum is added and plates are incubated at 35°C for 16-20 hours. MIC values are determined as the lowest concentration causing complete inhibition of visible growth. Quality control strains are included to ensure assay validity. DNA gyrase and topoisomerase IV inhibition assays are performed using purified enzymes and supercoiled DNA substrates.
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| Cell Assay |
Antibacterial activity is evaluated in bacterial cell cultures using standard microbiological methods. Broth microdilution assays are performed in 96-well plates with appropriate media. Bacteria are cultured to logarithmic phase and diluted to a standard inoculum. Orbifloxacin is serially diluted and added to wells. Plates are incubated at 35°C for 16-20 hours. MIC values are determined visually or using a microplate reader. Time-kill curve assays are performed to assess bactericidal activity. Each experiment includes quality control strains and antibiotic standards.
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| Animal Protocol |
In vivo efficacy of Orbifloxacin is evaluated in animal models of bacterial infection. The compound is administered orally or by injection at doses determined by veterinary studies. Bacterial burden is quantified in infected tissues by CFU plating. Clinical symptoms are monitored. Sample sizes typically range from 6-10 animals per group. Veterinary clinical studies have been conducted for various bacterial infections in livestock and domestic pets.
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| ADME/Pharmacokinetics |
Molecular Weight: 395.38. Formula: C19H20F3N3O3. CAS No.: 113617-63-3. CAS Name: rel-1-Cyclopropyl-7-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-5,6,8-trifluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid. Synonyms: 1-Cyclopropyl-5,6,8-trifluoro-1,4-dihydro-7-(cis-3,5-dimethyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic Acid. Appearance: White to orange to green powder to crystal. Purity: >98.0% (HPLC). Melting Point: 260°C (dec.). Storage: Room temperature (recommended in a cool and dark place, <15°C). Orbifloxacin is a synthetic fluoroquinolone antibacterial agent for veterinary use.
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| Toxicity/Toxicokinetics |
Orbifloxacin is generally well-tolerated in veterinary patients at therapeutic doses. Common adverse effects may include gastrointestinal disturbances and injection site reactions. As a fluoroquinolone, it may cause cartilage damage in young animals and should be used with caution in growing animals. The compound is for research use only and is not for human therapeutic use.
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| References | |
| Additional Infomation |
Orbifloxacin belongs to the quinolone class of drugs. Orbifloxacin is a fluoroquinolone antibiotic. It is marketed by Schering-Plough Animal Health and is approved for the treatment of certain infections in dogs. See also: Mometasone furoate; Orbifloxacin; Posaconazole (ingredients)... See more...
Orbifloxacin is also known as 1-Cyclopropyl-5,6,8-trifluoro-1,4-dihydro-7-(cis-3,5-dimethyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic Acid. Its CAS name is rel-1-Cyclopropyl-7-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-5,6,8-trifluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid. Orbifloxacin is a synthetic fluoroquinolone antibacterial agent developed as a veterinary chemotherapeutic for livestock and domestic pets. It exhibits in vitro activity against a wide range of Gram-positive and Gram-negative bacteria, enterobacteriaceae, anaerobes, and mycobacteria. The compound inhibits DNA gyrase and topoisomerase IV. Orbifloxacin is approved for veterinary use in many countries. |
| Molecular Formula |
C19H20F3N3O3
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| Molecular Weight |
395.38
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| Exact Mass |
395.145
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| Elemental Analysis |
C, 57.72; H, 5.10; F, 14.42; N, 10.63; O, 12.14
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| CAS # |
113617-63-3
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| PubChem CID |
60605
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
590.7±50.0 °C at 760 mmHg
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| Melting Point |
260 °C(dec.)
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| Flash Point |
311.1±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.588
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| LogP |
2.37
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
691
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@@H]1CN(C[C@@H](N1)C)C2=C(C3=C(C(=C2F)F)C(=O)C(=CN3C4CC4)C(=O)O)F
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| InChi Key |
QIPQASLPWJVQMH-DTORHVGOSA-N
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| InChi Code |
InChI=1S/C19H20F3N3O3/c1-8-5-24(6-9(2)23-8)17-14(21)13(20)12-16(15(17)22)25(10-3-4-10)7-11(18(12)26)19(27)28/h7-10,23H,3-6H2,1-2H3,(H,27,28)/t8-,9+
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| Chemical Name |
1-cyclopropyl-7-[(3R,5S)-3,5-dimethylpiperazin-1-yl]-5,6,8-trifluoro-4-oxoquinoline-3-carboxylic acid
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| Synonyms |
Orbifloxacin; ORBIFLOXACIN; 113617-63-3; Orbax; orbifloxacine; orbifloxacino; Orbax
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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 |
| 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) |
DMSO : ~6 mg/mL (~15.18 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5292 mL | 12.6461 mL | 25.2921 mL | |
| 5 mM | 0.5058 mL | 2.5292 mL | 5.0584 mL | |
| 10 mM | 0.2529 mL | 1.2646 mL | 2.5292 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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