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| 25g |
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| Targets |
Lomefloxacin inhibits bacterial DNA gyrase (a type II topoisomerase) and topoisomerase IV, enzymes essential for DNA replication and repair. This inhibition leads to decreased DNA synthesis during bacterial replication, resulting in cell growth inhibition and eventually cell lysis. These targets are specific to bacteria, providing selective toxicity.
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| ln Vitro |
Lomefloxacin demonstrates broad-spectrum antibacterial activity in vitro, inhibiting growth of various Gram-negative and Gram-positive bacteria including N. gonorrhoeae. The compound shows potent activity against urinary and respiratory pathogens. Minimum inhibitory concentration (MIC) values are determined for various bacterial strains to assess spectrum and potency.
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| ln Vivo |
Lomefloxacin is effective in vivo for treating bacterial infections such as bronchitis and urinary tract infections. It is orally bioavailable and has been used in clinical settings for these indications. The compound demonstrates in vivo efficacy against susceptible bacterial pathogens.
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| Enzyme Assay |
Non-cell-based enzyme assays for Lomefloxacin use purified DNA gyrase or topoisomerase IV enzymes. The compound is incubated with the enzyme, DNA substrate, and ATP. Enzyme activity is measured by assessing DNA supercoiling (for gyrase) or decatenation (for topoisomerase IV) using gel electrophoresis or fluorescence-based assays. IC50 values for enzyme inhibition are determined.
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| Cell Assay |
Cellular assays for Lomefloxacin involve broth microdilution or agar dilution methods to determine minimum inhibitory concentrations (MIC) against bacterial strains. Bacteria are cultured in appropriate medium and treated with the compound at varying concentrations. Bacterial growth is assessed by optical density measurement or colony counting after overnight incubation. MIC is defined as the lowest concentration inhibiting visible growth.
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| Animal Protocol |
In vivo animal models for Lomefloxacin include standard infection models such as murine urinary tract infection or pneumonia models. Animals are inoculated with pathogenic bacteria, then treated with the compound via oral or parenteral routes. Efficacy is assessed by bacterial burden in target organs, survival rates, and clinical signs of infection. Detailed protocols are not extensively reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Lomefloxacin hydrochloride include molecular weight of 387.81 g/mol and molecular formula C17H19ClF2N3O3. The compound is orally bioavailable. Purity ranges from 99.43% to 99.75%. It appears as a white powder. Detailed PK parameters such as half-life and bioavailability are typical of fluoroquinolone antibiotics.
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| Toxicity/Toxicokinetics |
Lomefloxacin hydrochloride has been used clinically for treating bronchitis and urinary tract infections. As a fluoroquinolone, potential adverse effects include gastrointestinal disturbances, CNS effects, and tendon toxicity. The compound is for research and clinical use. Detailed toxicity data are available from clinical experience but not extensively detailed in the provided sources.
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| References |
:J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Oct15;878(28):2937-41;Pak J Pharm Sci. 2005Jul;18(3):59-65.
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| Additional Infomation |
Lomefloxacin hydrochloride is the hydrochloride salt of lomefloxacin. It is taken orally to treat bacterial infections, including bronchitis and urinary tract infections. It can also be used topically as eye drops for bacterial conjunctivitis and as ear drops for otitis externa and otitis media. It has photosensitizing, antibacterial, and antituberculosis effects. It contains lomefloxacin. Lomefloxacin hydrochloride is the hydrochloride form of lomefloxacin, a synthetic broad-spectrum fluoroquinolone antibacterial drug. Lomefloxacin hydrochloride inhibits DNA gyrase, a type II topoisomerase involved in the induction or relaxation of supercoiling during DNA replication. This inhibition leads to reduced DNA synthesis during bacterial replication, thereby inhibiting cell growth and ultimately causing cell lysis. See also: Lomefloxacin (with active fraction).
Lomefloxacin hydrochloride is also known as Okacyn. It has CAS number 98079-52-8. The compound is a fluoroquinolone antibiotic that inhibits DNA gyrase and topoisomerase IV. It is used for treating urinary tract and respiratory infections. Purity is high (99.43-99.75%) and it is available as a white powder. |
| Molecular Formula |
C17H20CLF2N3O3
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|---|---|
| Molecular Weight |
387.81
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| Exact Mass |
387.116
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| Elemental Analysis |
C, 52.65; H, 5.20; Cl, 9.14; F, 9.80; N, 10.84; O, 12.38
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| CAS # |
98079-52-8
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| Related CAS # |
Lomefloxacin-d5 hydrochloride;Lomefloxacin;98079-51-7;Lomefloxacin (aspartate);211690-33-4
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| PubChem CID |
68624
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| Appearance |
White to off-white solid powder
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| Boiling Point |
542.7ºC at 760 mmHg
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| Melting Point |
290-3000C
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| Flash Point |
282ºC
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| LogP |
2.991
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
586
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].FC1=C2C(C(C(C(=O)O[H])=C([H])N2C([H])([H])C([H])([H])[H])=O)=C([H])C(=C1N1C([H])([H])C([H])([H])N([H])C([H])(C([H])([H])[H])C1([H])[H])F
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| InChi Key |
KXEBLAPZMOQCKO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H19F2N3O3.ClH/c1-3-21-8-11(17(24)25)16(23)10-6-12(18)15(13(19)14(10)21)22-5-4-20-9(2)7-22;/h6,8-9,20H,3-5,7H2,1-2H3,(H,24,25);1H
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| Chemical Name |
1-ethyl-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid;hydrochloride
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| Synonyms |
Lomefloxacin hydrochloride; Lomefloxacin HCl; Maxaquin; Ny-198; Bareon; Pharmacia Brand 1 of Lomefloxacin Hydrochloride; Pharmacia Brand 2 of Lomefloxacin Hydrochloride; SC 4711; SC-4711;
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
Water : 7.14~6 mg/mL(~18.41 mM)
DMSO : ~1 mg/mL ( ~2.57 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 | 2.5786 mL | 12.8929 mL | 25.7858 mL | |
| 5 mM | 0.5157 mL | 2.5786 mL | 5.1572 mL | |
| 10 mM | 0.2579 mL | 1.2893 mL | 2.5786 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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