| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
| ln Vitro |
Balofloxacin (25 mg/mL; 1 hour) decreases the development of Staphylococcus aureus adhering to human corneal epithelial cells (HCEC) [2]. Balofloxacin inhibits Staphylococcus aureus ATCC 25923 with a MIC of 0.125 mg/mL[2]. Balofloxacin (0.05-500 μg/mL; 72 hours) is not harmful to HCEC at low concentrations (eg, 0.625 mg/mL) [2].
- Cytotoxicity in HCECs: Balofloxacin exhibited low cytotoxicity against human corneal epithelial cells (HCECs) in a concentration-dependent manner. At low concentrations (e.g., 0.625 µg/mL), no toxicity was observed. Its cytotoxicity was significantly greater than levofloxacin only at 1.25 µg/mL (P<0.05). At concentrations higher than 2.5 µg/mL, there was no significant difference in cell viability between balofloxacin and levofloxacin. [2] - Antibiotic Susceptibility (MIC): The minimal inhibitory concentration (MIC) of balofloxacin against Staphylococcus aureus ATCC 25923 was determined to be 0.125 µg/mL, which was the same as that for levofloxacin. [2] - Bacterial Susceptibility in Infected Cells: In HCECs infected with S. aureus, treatment with balofloxacin at 25 µg/mL for 1 hour significantly reduced the number of viable bacteria (colony-forming units, CFU) compared to the untreated control (P<0.001). Morphological observation showed hardly any bacterial growth in balofloxacin-treated cells. Balofloxacin was significantly more effective in reducing bacterial CFU than levofloxacin under the same conditions (P<0.001). [2] |
|---|---|
| ln Vivo |
Balofloxacin (200 mg/kg/day; orally for 5 days) decreases the amount of viable Mycoplasma pneumoniae in hamster lungs [3]. Rabbits with bacterial keratitis caused by Staphylococcus aureus can effectively treat their eye infections with 0.5% balofloxacin [2].
- Efficacy in Experimental Bacterial Keratitis (Rabbit Model): Topical treatment with balofloxacin eye drops (0.5%) in a rabbit model of S. aureus keratitis significantly improved clinical scores compared to the baseline (infected, untreated at 16h) and phosphate-buffered saline (PBS) control groups (P=0.011 for both). The median total clinical score in the balofloxacin group was 10 (range 8-20), which was significantly lower than that in the levofloxacin group [15 (6-20), P=0.007]. [2] - Histopathological Improvement: Corneas from the balofloxacin-treated group showed only slight stromal edema and no significant inflammatory cell infiltration. A small amount of inflammatory cells was observed in the anterior chamber and angle. This outcome was better than that in the levofloxacin-treated group and markedly better than the control groups. [2] - Microbiological Evaluation (Corneal CFU): Treatment with balofloxacin eye drops (0.5%) resulted in a significantly lower number of CFU recovered from infected corneas compared to the PBS control group (P<0.001) and the levofloxacin treatment group (P=0.010). The levofloxacin group did not show a significant reduction in CFU compared to the control (P=0.597). [2] |
| Cell Assay |
- Corneal Epithelial Cell Viability (MTT) Assay: Human corneal epithelial cells (HCECs) were seeded at 3,000 cells/well in 96-well plates and cultured for 2 days. The cells were then exposed to serially diluted solutions of balofloxacin in culture medium for 72 hours. After exposure, cell viability was quantified using the MTT assay. The absorbance, proportional to the number of viable cells, was measured. Cell viability in test solutions was calculated as a percentage relative to cells incubated in growth medium without the drug. [2]
- Bacterial Susceptibility in Cell Culture: HCECs were cultured in 24-well plates. After reaching confluence, cells were incubated with serum-free medium for 12 hours. Subsequently, 100 µL of a S. aureus suspension (10^9 cells/mL) was added to each well and incubated for 1 hour to allow infection. The wells were then washed with PBS to remove non-adherent bacteria. The infected cells were treated with balofloxacin-containing medium at a concentration of 25 µg/mL for 1 hour. After treatment, cells from some wells were fixed for microscopic observation. Cells from other wells were detached using a trypsin-EDTA and Triton X-100 mixture, serially diluted, plated on agar plates, and incubated for 24 hours at 37°C to determine the number of colony-forming units (CFU). [2] |
| Animal Protocol |
- Rabbit Model of Bacterial Keratitis and Treatment: New Zealand White rabbits were systemically anesthetized. After topical anesthesia, 5 µL of a S. aureus suspension containing 100 CFU was injected into the corneal stroma of each eye using a micro-syringe to induce keratitis. Sixteen hours post-infection, rabbits with established infections were randomly divided into treatment groups. The balofloxacin treatment group received balofloxacin eye drops (0.5%). The eye drops were formulated as a 0.5% sterilized water solution containing balofloxacin 5 mg/mL. The pH was first adjusted to approximately 8.5 with sodium hydroxide to dissolve the drug, then adjusted to approximately 6.35 with hydrochloric acid, and the osmolality was adjusted to approximately 300 mOsm with sodium chloride. The treatment regimen consisted of administering one drop to each eye every 15 minutes for 5 doses, followed by one drop every 30 minutes for 14 doses (a total of 19 doses over 8 hours). Clinical examinations and sample collection (for histology and CFU counting) were performed 1 hour after the last dose. [2]
|
| Toxicity/Toxicokinetics |
In vitro cytotoxicity: As described in the in vitro experiments section, balofloxacin exhibits concentration-dependent cytotoxicity to human corneal endothelial cells (HCECs), but is similar to that of levofloxacin at clinically relevant concentrations. The cytotoxicity of 0.5% balofloxacin eye drops formulation after exposure for 5, 10, or 30 minutes is similar to that of commercially available 0.5% levofloxacin eye drops, indicating that short-term ocular exposure is safe. [2]
|
| References | |
| Additional Infomation |
See also: Balofloxacin (note moved to). Balofloxacin is a novel fluoroquinolone antibiotic with broad-spectrum antibacterial activity against Gram-positive, Gram-negative, and anaerobic bacteria. It has been reported to have a higher affinity for bacterial topoisomerase IV. [2] Balofloxacin is currently used orally for the treatment of respiratory, intestinal, and urinary tract infections, but at the time of this study, no ophthalmic formulation was publicly available. This study aimed to evaluate its potential for topical ophthalmic use. [2] The study concluded that balofloxacin eye drops (0.5%) were safe for corneal epithelial cells and more effective than levofloxacin eye drops (0.5%) in treating experimental Staphylococcus aureus keratitis in rabbits, suggesting its potential clinical value in ophthalmology. [2]
|
| Molecular Formula |
C20H28FN3O6
|
|---|---|
| Molecular Weight |
425.4512
|
| Exact Mass |
425.196
|
| CAS # |
151060-21-8
|
| Related CAS # |
Balofloxacin;127294-70-6
|
| PubChem CID |
6918202
|
| Appearance |
Typically exists as solid at room temperature
|
| Melting Point |
135 °C
|
| LogP |
2.697
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
30
|
| Complexity |
668
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC1C([H])=C2C(C(C(=O)O[H])=C([H])N(C2=C(C=1N1C([H])([H])C([H])([H])C([H])([H])C([H])(C1([H])[H])N([H])C([H])([H])[H])OC([H])([H])[H])C1([H])C([H])([H])C1([H])[H])=O.O([H])[H].O([H])[H]
|
| InChi Key |
WEGNYJXOCPJAPS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H24FN3O4.2H2O/c1-22-11-4-3-7-23(9-11)17-15(21)8-13-16(19(17)28-2)24(12-5-6-12)10-14(18(13)25)20(26)27;;/h8,10-12,22H,3-7,9H2,1-2H3,(H,26,27);2*1H2
|
| Chemical Name |
1-cyclopropyl-6-fluoro-8-methoxy-7-[3-(methylamino)piperidin-1-yl]-4-oxoquinoline-3-carboxylic acid;dihydrate
|
| 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 (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.3505 mL | 11.7523 mL | 23.5045 mL | |
| 5 mM | 0.4701 mL | 2.3505 mL | 4.7009 mL | |
| 10 mM | 0.2350 mL | 1.1752 mL | 2.3505 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
