| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg | |||
| Other Sizes |
| Targets |
Nemonoxacin targets bacterial DNA gyrase and topoisomerase IV, enzymes essential for bacterial DNA replication and transcription. As a non-fluorinated quinolone, it inhibits these enzymes by stabilizing the enzyme-DNA cleavage complex, leading to bacterial cell death.
|
|---|---|
| ln Vitro |
Nemonoxacin exhibits antibacterial activity against Chlamydia pneumoniae, as evidenced by a MIC90 of 0.06 μg/mL [1]. While vancomycin MRSA (MIC90) has limited effectiveness at 2 μg/ml, nemofloxacin is extremely active against community-acquired MRSA (CA-MRSA) (MIC90: 0.5 and 0.06 μg/ml) and intermediate against ciprofloxacin-resistant MRSA (MIC90: 1 μg/ml) [2].
Nemonoxacin has potent antibacterial activity against a wide range of pathogens. It has activity against Chlamydia pneumoniae with MIC90s of 0.06 μg/mL. Nemonoxacin is highly active against community-acquired MRSA (CA-MRSA) with an MIC90 of 0.5 μg/mL. It also inhibits drug-resistant Streptococcus pneumoniae and methicillin-resistant Staphylococcus aureus. |
| ln Vivo |
Nemonoxacin has been approved for the treatment of community-acquired pneumonia, demonstrating clinical efficacy in patients. Its broad-spectrum activity against Gram-positive, Gram-negative, and atypical pathogens supports its use in respiratory tract infections.
|
| Enzyme Assay |
The antibacterial activity of nemonoxacin can be assessed using standard broth microdilution or agar dilution methods according to CLSI guidelines. Bacterial strains are cultured in appropriate media and exposed to serial two-fold dilutions of nemonoxacin. After overnight incubation at 35°C, the minimum inhibitory concentration (MIC) is determined as the lowest concentration that visibly inhibits bacterial growth.
|
| Cell Assay |
Nemonoxacin's antibacterial activity is evaluated in vitro using a panel of Gram-positive, Gram-negative, and atypical bacterial strains. Broth microdilution or agar dilution methods are performed to determine MIC values. Time-kill kinetics and post-antibiotic effect studies can also be conducted to characterize the bactericidal activity of the compound.
|
| Animal Protocol |
Nemonoxacin is administered orally for the treatment of community-acquired pneumonia. In preclinical studies, the compound would be evaluated in animal models of bacterial infection, such as murine pneumonia or sepsis models. Efficacy is assessed by measuring survival rates, bacterial load in target organs, and clinical signs of infection.
|
| ADME/Pharmacokinetics |
Nemonoxacin Malate has a molecular weight of 505.52 and a molecular formula of C24H31N3O9. It is a non-fluorinated quinolone antibiotic. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources for the malate salt form.
|
| Toxicity/Toxicokinetics |
Nemonoxacin is generally well-tolerated. As a quinolone antibiotic, potential adverse effects may include gastrointestinal disturbances, central nervous system effects, and tendinopathy. The non-fluorinated structure may offer an improved safety profile compared to fluorinated quinolones. Specific LD50 values are not extensively detailed.
|
| References |
[1]. Chotikanatis K, et al. In vitro activity of nemonoxacin, a novel nonfluorinated quinolone antibiotic, against Chlamydia trachomatis and Chlamydia pneumoniae. Antimicrob Agents Chemother. 2014;58(3):1800-1.
[2]. Lai CC, et al. Nemonoxacin (TG-873870) for treatment of community-acquired pneumonia. Expert Rev Anti Infect Ther. 2014 Apr;12(4):401-17. |
| Additional Infomation |
Nemonoxacin Malate (CAS# 951163-60-3) is also known as TG-873870. It is a non-fluorinated quinolone antibiotic approved for the treatment of community-acquired pneumonia under the brand name Taigexyn. It exhibits potent activity against MRSA and fluoroquinolone-resistant strains.
|
| Molecular Formula |
C24H31N3O9
|
|---|---|
| Molecular Weight |
505.51764
|
| Exact Mass |
505.206
|
| CAS # |
951163-60-3
|
| Related CAS # |
Nemonoxacin;378746-64-6
|
| PubChem CID |
49863435
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.888
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
36
|
| Complexity |
776
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
OC(CC(C(=O)O)O)=O.C[C@H]1C[C@H](N)CN(C2C=CC3=C(N(C4CC4)C=C(C3=O)C(=O)O)C=2OC)C1
|
| InChi Key |
YMVJINCWEIPOFL-FXMYHANSSA-N
|
| InChi Code |
InChI=1S/C20H25N3O4.C4H6O5/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;5-2(4(8)9)1-3(6)7/h5-6,10-13H,3-4,7-9,21H2,1-2H3,(H,25,26);2,5H,1H2,(H,6,7)(H,8,9)/t11-,12-;/m0./s1
|
| Chemical Name |
7-((3S,5S)-3-amino-5-methylpiperidin-1-yl)-1-cyclopropyl-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid malate
|
| Synonyms |
TG-873870 TG873870 TG 873870 Nemonoxacin Malate
|
| HS Tariff Code |
2934.99.9001
|
| 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, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~197.82 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9782 mL | 9.8908 mL | 19.7816 mL | |
| 5 mM | 0.3956 mL | 1.9782 mL | 3.9563 mL | |
| 10 mM | 0.1978 mL | 0.9891 mL | 1.9782 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
