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| Targets |
Nemonoxacin targets bacterial DNA gyrase and topoisomerase IV, which are essential enzymes for bacterial DNA replication, transcription, repair, and recombination. By inhibiting these enzymes, it prevents bacterial cell division and leads to cell death. Its unique structure, lacking fluorine at the C-8 position, contributes to its activity against fluoroquinolone-resistant strains.
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| ln Vitro |
Nemonoxacin has strong antibacterial action in vitro (0–5.51 µM; 24 hours) [1].
In vitro, Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenzae. It inhibits MSSA and MRSA with MIC50 values of 0.12 and 4 µg/mL, respectively. The compound has demonstrated activity against a wide range of pathogens, including Streptococcus pneumoniae and various Enterobacteriaceae. |
| ln Vivo |
Nemonoxacin (oral; 15 minutes and 6 hours after infection) has been demonstrated to be effective against Gram-positive bacteria (Staphylococcus aureus, Staphylococcus capitis, Streptococcus pneumoniae, and Enterococcus faecalis) and Gram-negative bacteria (E. coli) and broad-spectrum in vivo activity. Escherichia coli) isolation [2]. Nemonoxacin (oral; 6, 12, and 24 hours post-infection) has been proven to be efficacious against (2.5, 5, 10, 20 mg/kg) Streptococcus pneumoniae 0613 (PRSP) and (10, 20, 40, 80 mg/kg) K Activity. Pneumonia 0607 infected mouse lung infection model [2].
In vivo, Nemonoxacin has demonstrated potent and broad-spectrum activity in mouse models of infection. In a mouse systemic infection model, oral administration of Nemonoxacin 15 minutes and 6 hours after infection was effective against Gram-positive (S. aureus, S. capitis, S. pneumonia, E. faecalis) and Gram-negative (E. coli) isolates. It also showed potent activity against S. pneumonia and K. pneumonia infections in a mouse pulmonary infection model. |
| Enzyme Assay |
In vitro assays for Nemonoxacin involve determining its minimum inhibitory concentration (MIC) against various bacterial strains. Bacteria are cultured in the presence of varying concentrations of the compound (0-5.51 μM) for 24 hours. The MIC50 values are determined by assessing bacterial growth inhibition.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: MSSA, MRSA Tested Concentrations: 0-5.51 µM (0-2048 µg/mL) Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of MSSA and MRSA with MIC90 values of 0.12 and 4 µg/mL. |
| Animal Protocol |
Animal/Disease Models: CD-1 ICR mouse (18-22 grams; mouse systemic infection model) [2].
Doses: 1.6-4.0 mg/kg (Staphylococcus aureus and Streptococcus capitis infection), 2.4-10.0 mg/kg (Streptococcus pneumoniae infection), 5.0-22.6 mg/kg (Enterococcus faecalis infection), 1.6-10.0 mg/kg kg (E. coli infection) Route of Administration: Oral; 15 minutes and 6 hrs (hrs (hours)) post-infection Experimental Results: Against Staphylococcus aureus ATCC 29213 (MSSA), Staphylococcus aureus 0705 (MRSA) and Staphylococcus capitis 0687 ( The ED50 of levofloxacin-resistant MRSC) were 2.08, 2.59 and 2.52 mg/kg, respectively. Animal/Disease Models: CD-1 ICR mouse (18-22 grams; mouse lung infection model) [2]. Doses: 2.5, 5, 10, 20 mg/kg (Streptococcus pneumoniae 0613 (PRSP)); 10, 20, 40, 80 mg/kg (Klebsiella pneumoniae 0607) Route of Administration: Oral; 6, 12 after infection and 24-hour Experimental Results: significant reduction in body colony count. In vivo animal studies for Nemonoxacin are conducted in CD-1 ICR mice (18-22 g) using a systemic infection model. The compound is administered orally at various doses (1.6-80 mg/kg) 15 minutes and 6 hours after infection. Efficacy is assessed by measuring the survival rate of the mice or by quantifying bacterial load in target organs. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Nemonoxacin are not detailed in the provided sources. The compound is orally active and is soluble in DMSO. Powder formulations should be stored at -20°C for up to 3 years. It is available as a pharmaceutical product (Taigexyn®) in some regions.
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| Toxicity/Toxicokinetics |
Nemonoxacin is generally well-tolerated. As a quinolone antibiotic, it may have class-related side effects. Specific toxicological data are not provided in the available sources. The compound is intended for the treatment of bacterial infections.
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| References |
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| Additional Infomation |
Nemonoxacin belongs to the quinoline class of drugs.
Drug Indications It has been studied for the treatment of bacterial infections and pneumonia. Nemonoxacin is a novel non-fluorinated quinolone antibiotic with broad-spectrum activity. It is being investigated for the treatment of bacterial infections and community-acquired pneumonia. The compound is particularly effective against drug-resistant strains such as MRSA. It is available from commercial suppliers for research purposes. |
| Molecular Formula |
C20H25N3O4
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| Molecular Weight |
371.4302
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| Exact Mass |
371.185
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| CAS # |
378746-64-6
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| Related CAS # |
Nemonoxacin malate;951163-60-3;Nemonoxacin-d3;Nemonoxacin-d3-1;Nemonoxacin-d4
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| PubChem CID |
11993740
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| Appearance |
White to off-white solid powder
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| LogP |
2.982
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
647
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@H]1C[C@@H](CN(C1)C2=C(C3=C(C=C2)C(=O)C(=CN3C4CC4)C(=O)O)OC)N
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| InChi Key |
AVPQPGFLVZTJOR-RYUDHWBXSA-N
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| InChi Code |
InChI=1S/C20H25N3O4/c1-11-7-12(21)9-22(8-11)16-6-5-14-17(19(16)27-2)23(13-3-4-13)10-15(18(14)24)20(25)26/h5-6,10-13H,3-4,7-9,21H2,1-2H3,(H,25,26)/t11-,12-/m0/s1
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| Chemical Name |
7-[(3S,5S)-3-amino-5-methylpiperidin-1-yl]-1-cyclopropyl-8-methoxy-4-oxoquinoline-3-carboxylic acid
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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) |
DMSO : ~2 mg/mL (~5.38 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 | 2.6923 mL | 13.4615 mL | 26.9230 mL | |
| 5 mM | 0.5385 mL | 2.6923 mL | 5.3846 mL | |
| 10 mM | 0.2692 mL | 1.3461 mL | 2.6923 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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