| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Bacterial DNA topoisomerase (DNA gyrase and topoisomerase IV). As a non-fluorinated quinolone antibiotic, Nemonoxacin targets bacterial DNA replication by inhibiting these essential enzymes, ultimately leading to bacterial cell death.
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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[4].
In vitro, Nemonoxacin exhibits potent antibacterial activity against a broad spectrum of Gram-positive and Gram-negative pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and quinolone-resistant strains. Its MIC90 values are typically <1 ug/mL for susceptible organisms. The non-fluorinated structure contributes to a reduced potential for selecting resistant mutants. |
| ln Vivo |
Nemonoxacin demonstrates good in vivo efficacy in animal models of bacterial infection, including murine models of pneumonia and septicemia. Oral administration results in significant reduction of bacterial load in target tissues. Its efficacy is comparable to or better than that of levofloxacin and moxifloxacin in some models.
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| Enzyme Assay |
The non-cellular enzyme inhibition assays for Nemonoxacin involve measuring the inhibition of DNA supercoiling activity of purified DNA gyrase or the decatenation activity of topoisomerase IV. The assay uses a reaction mixture containing the enzyme, a relaxed plasmid DNA substrate, ATP, and serial dilutions of the compound. After incubation, the reaction is stopped, and the products are resolved by agarose gel electrophoresis. The concentration required to inhibit 50% of the enzymatic activity (IC50) is calculated.
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| Cell Assay |
For in vitro cellular assays, bacterial strains are cultured in appropriate media to mid-log phase. The minimum inhibitory concentration (MIC) is determined using the broth microdilution method according to CLSI guidelines. Serial two-fold dilutions of Nemonoxacin are prepared in 96-well plates, and a standardized bacterial inoculum is added. Plates are incubated at 35degC for 16-20 hours, and the MIC is defined as the lowest concentration that prevents visible bacterial growth.
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| Animal Protocol |
For in vivo efficacy studies, a murine systemic infection model is used. Female ICR mice are inoculated intraperitoneally with a lethal dose of bacterial suspension. Nemonoxacin is administered orally at various doses at 1 and 5 hours post-infection. Survival rates are monitored for 7 days, and the 50% effective dose (ED50) is calculated. Alternatively, a neutropenic murine thigh infection model can be used, where bacterial colony counts in thigh homogenates are determined after 24 hours of treatment.
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| ADME/Pharmacokinetics |
In rats, Nemonoxacin shows good oral bioavailability (>70%), a moderate half-life (t1/2 ~4-6 hours), and low plasma protein binding. It penetrates well into lung tissues, achieving high concentrations that are several-fold above the MIC for target pathogens. The major route of excretion is via the kidneys, with a significant portion of the dose recovered unchanged in urine.
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| Toxicity/Toxicokinetics |
Nemonoxacin is generally well-tolerated in preclinical safety studies. No significant phototoxicity or central nervous system side effects have been observed, which are common concerns with some quinolone antibiotics. In repeated-dose toxicity studies, the no-observed-adverse-effect level (NOAEL) was established at doses several-fold higher than the therapeutic exposure.
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| References |
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| Additional Infomation |
The stable heavy isotope (deuterium) labeling of Nemonoxacin-d3 does not alter its biological activity but serves as an internal standard for accurate LC-MS/MS quantification in pharmacokinetic and metabolism studies. Nemonoxacin has completed Phase II clinical trials for community-acquired pneumonia (CAP) and has been granted approval in some regions, though not by the U.S. FDA.
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| Molecular Formula |
C20H22D3N3O4
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|---|---|
| Molecular Weight |
374.45
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| Related CAS # |
Nemonoxacin;378746-64-6
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| Appearance |
Off-white to light yellow solid powder
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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 | 2.6706 mL | 13.3529 mL | 26.7058 mL | |
| 5 mM | 0.5341 mL | 2.6706 mL | 5.3412 mL | |
| 10 mM | 0.2671 mL | 1.3353 mL | 2.6706 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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