| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary molecular targets of levofloxacin sodium are bacterial DNA gyrase (topoisomerase II) and topoisomerase IV. It binds to these enzymes and inhibits their activity, blocking DNA replication and repair. DNA gyrase is responsible for introducing negative supercoils into DNA, while topoisomerase IV is involved in decatenation of daughter chromosomes after replication. By inhibiting both enzymes, levofloxacin sodium disrupts bacterial DNA metabolism, leading to bacterial cell death. It shows enhanced activity against Streptococcus pneumoniae compared to earlier fluoroquinolones.
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|---|---|
| ln Vitro |
In vitro, levofloxacin sodium inhibits DNA gyrase and topoisomerase IV with IC50 values in the microgram per milliliter range. It exhibits broad-spectrum antibacterial activity against Gram-positive and Gram-negative bacteria. It is particularly active against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. Its in vitro activity is measured using standard broth microdilution MIC testing according to CLSI guidelines. It also shows activity against atypical pathogens such as Mycoplasma and Chlamydia.
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| ln Vivo |
In vivo, levofloxacin sodium is effective in treating respiratory tract infections, urinary tract infections, and skin infections. It achieves high concentrations in lung tissue and is effective against penicillin-resistant Streptococcus pneumoniae. Its in vivo efficacy is dose-dependent and correlates with AUC/MIC ratios. It is well absorbed after oral administration and has excellent tissue penetration. Its pharmacokinetic properties include a half-life of 6-8 hours and 87% bioavailability.
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| Enzyme Assay |
For DNA gyrase inhibition assays, purified DNA gyrase from E. coli or Streptococcus pneumoniae is incubated with supercoiled plasmid DNA and levofloxacin sodium at various concentrations. The reaction is incubated at 37°C for 30-60 minutes, and DNA supercoiling is analyzed by agarose gel electrophoresis. IC50 values are determined by quantifying the conversion of relaxed to supercoiled DNA. For topoisomerase IV assays, decatenation of kinetoplast DNA is measured.
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| Cell Assay |
For in vitro cell experiments, bacterial cultures are grown in Mueller-Hinton broth and treated with levofloxacin sodium at concentrations ranging from 0.001-10 μg/mL. The MIC is determined by broth microdilution according to CLSI guidelines. For time-kill studies, bacterial cultures are incubated with the compound, and viable counts are determined at various time points. For resistance studies, serial passage in sub-inhibitory concentrations is performed.
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| Animal Protocol |
For in vivo animal experiments, mice or rats are used. Levofloxacin sodium is administered by oral gavage or intravenous injection at doses ranging from 1-50 mg/kg/day for 3-7 days. For respiratory infection models, animals are infected with Streptococcus pneumoniae by intranasal inoculation, and bacterial burden in lungs is quantified. For urinary tract infection models, animals are infected by intravesical inoculation. Pharmacokinetic parameters are determined by LC-MS/MS.
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| References |
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| Molecular Formula |
C18H19FN3NAO4
|
|---|---|
| Molecular Weight |
383.349338769913
|
| Exact Mass |
383.126
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| CAS # |
872606-49-0
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| Related CAS # |
Levofloxacin;100986-85-4;(R)-Ofloxacin;100986-86-5
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| PubChem CID |
71300639
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
0.212
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
640
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[Na+].FC1C=C2C(C(C(=O)[O-])=CN3C2=C(C=1N1CCN(C)CC1)OC[C@@H]3C)=O
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| InChi Key |
NCGMIBYQHQSCGQ-PPHPATTJSA-M
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| InChi Code |
InChI=1S/C18H20FN3O4.Na/c1-10-9-26-17-14-11(16(23)12(18(24)25)8-22(10)14)7-13(19)15(17)21-5-3-20(2)4-6-21;/h7-8,10H,3-6,9H2,1-2H3,(H,24,25);/q;+1/p-1/t10-;/m0./s1
|
| Chemical Name |
sodium;(2S)-7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylate
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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) |
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
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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 | 2.6086 mL | 13.0429 mL | 26.0858 mL | |
| 5 mM | 0.5217 mL | 2.6086 mL | 5.2172 mL | |
| 10 mM | 0.2609 mL | 1.3043 mL | 2.6086 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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