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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Lomefloxacin targets bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, enzymes essential for DNA replication, transcription, and repair. Lomefloxacin-d5 has the same mechanism of action but is used as a tracer.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[3].
Lomefloxacin (unlabeled) is a fluoroquinolone antibiotic with broad-spectrum activity against Gram-negative and some Gram-positive bacteria. Lomefloxacin-d5 is expected to have the same biological activity but is not used for its therapeutic effects. |
| ln Vivo |
Lomefloxacin (unlabeled) is used to treat bacterial infections including bronchitis, urinary tract infections, and gastrointestinal infections. Lomefloxacin-d5 is not used for its therapeutic effects but as a tracer.
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| Enzyme Assay |
Non-cell assays for lomefloxacin-d5 are not performed due to its use as an internal standard. However, the parent compound, lomefloxacin, can be studied in bacterial enzyme assays. Purified DNA gyrase (topoisomerase II) is incubated with lomefloxacin in the presence of ATP and supercoiled plasmid DNA. The inhibition of DNA supercoiling is analyzed by agarose gel electrophoresis and visualized by ethidium bromide staining.
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| Cell Assay |
Lomefloxacin-d5 is not used in cellular assays for its antibacterial effects. The unlabeled parent compound is used for antimicrobial susceptibility testing. The minimum inhibitory concentration (MIC) of lomefloxacin against a panel of bacteria can be determined using the broth microdilution method per CLSI guidelines. As a stable isotope-labeled internal standard, lomefloxacin-d5 is added to biological samples (e.g., plasma, urine, tissue homogenates) at a fixed concentration (e.g., 10-100 ng/mL). The samples are then prepared for LC-MS/MS analysis.
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| Animal Protocol |
In vivo studies are not performed with lomefloxacin-d5 as a therapeutic. It is used in pharmacokinetic studies as an internal standard. In such studies, the unlabeled parent drug (lomefloxacin) is administered to animals. Blood and tissue samples are collected, and lomefloxacin-d5 is added to these samples as an internal standard before LC-MS/MS analysis.
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| ADME/Pharmacokinetics |
Lomefloxacin-d5 is a stable isotope-labeled compound used as an internal standard. Its pharmacokinetics are not directly measured. The unlabeled parent drug, lomefloxacin, has an oral bioavailability of 95-98% in humans. It is widely distributed, with a volume of distribution of 1.5-2 L/kg. Plasma protein binding is about 30%. The elimination half-life is 7-9 hours. The deuterated version is expected to have a similar PK profile but is not used for therapeutic purposes.
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| Toxicity/Toxicokinetics |
The unlabeled lomefloxacin is generally well-tolerated. Common adverse effects include nausea, diarrhea, headache, and dizziness. More serious effects include photosensitivity, tendonitis, and QT prolongation. Lomefloxacin-d5 is used at very low concentrations (ng/mL level) as an internal standard, posing no significant toxicological risk.
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| References |
[1]. Hoogkamp-Korstanje JA. In-vitro activities of ciprofloxacin, levofloxacin, lomefloxacin, ofloxacin, pefloxacin, sparfloxacin and trovafloxacin against gram-positive and gram-negative pathogens from respiratory tract infections. J Antimicrob Chemother. 1997 Sep;40(3):427-31.
[2]. Reem I Al-Wabli. Lomefloxacin. Profiles Drug Subst Excip Relat Methodol. 2017;42:193-240. [3]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223. |
| Additional Infomation |
Lomefloxacin-d5 hydrochloride is a stable isotope-labeled research compound. It is used primarily as an internal standard in LC-MS/MS methods for the accurate quantification of lomefloxacin in biological samples. It is strictly for research use and is not for human consumption. The incorporation of five deuterium atoms distinguishes the labeled drug from the unlabeled form.
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| Molecular Formula |
C17H15D5CLF2N3O3
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| Related CAS # |
Lomefloxacin hydrochloride;98079-52-8
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| Appearance |
Typically exists as solid at room temperature
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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.) |
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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