Linezolid (Synonyms: PNU 100766) |
| رقم الكتالوجGC11221 |
Linezolid (PNU-100766) هو أول عضو في فئة المضادات الحيوية الاصطناعية Oxazolidinone.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 165800-03-3
Sample solution is provided at 25 µL, 10mM.
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Linezolid (PNU-100766) is an orally active oxazolidinone antibiotic that has inhibitory activity against a variety of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), glycopeptide-intermediate Staphylococcus aureus (GISA), vancomycin-resistant Enterococci (VRE), and penicillin-resistant Streptococcus pneumoniae[1]. Linezolid is a 50S ribosomal subunit-specific inhibitor that binds to the 50S ribosomal subunit to inhibit the initial step of protein synthesis[2]. The IC50 of linezolid for protein synthesis in Staphylococcus aureus is 0.3μg/ml, and the IC50 for 50S subunit formation is 0.6μg/ml[3]. Linezolid is indicated for the treatment of skin infections, bacterial pneumonia, and infections complicated by bacteremia[4].
In vitro, Linezolid (1.18 mM) treatment of THP-1 cells infected with Staphylococcus aureus (ATCC 25923 and E19977) for 24 h had no effect on cell viability, but had a significant inhibitory effect on intracellular and extracellular strains[5].
In vivo, Linezolid (50 mg/kg) was intraperitoneally injected into rats with MRSA mediastinitis for 7 days, significantly reducing bacterial counts in the mediastinum and sternum[6].
References:
[1] Perry C M, Jarvis B. Linezolid: a review of its use in the management of serious gram-positive infections[J]. Drugs, 2001, 61: 525-551.
[2] Swaney S M, Aoki H, Ganoza M C, et al. The oxazolidinone linezolid inhibits initiation of protein synthesis in bacteria[J]. Antimicrobial agents and chemotherapy, 1998, 42(12): 3251-3255.
[3] Champney W S, Miller M. Linezolid is a specific inhibitor of 50S ribosomal subunit formation in Staphylococcus aureus cells[J]. Current microbiology, 2002, 44: 350-356.
[4] Chen H, Du Y, Xia Q, et al. Role of linezolid combination therapy for serious infections: review of the current evidence[J]. European Journal of Clinical Microbiology & Infectious Diseases, 2020, 39: 1043-1052.
[5] Sandberg A, Jensen K S, Baudoux P, et al. Intra-and extracellular activity of linezolid against Staphylococcus aureus in vivo and in vitro[J]. Journal of antimicrobial chemotherapy, 2010, 65(5): 962-973.
[6] Sacar M, Sacar S, Kaleli I, et al. Efficacy of linezolid in the treatment of mediastinitis due to methicillin-resistant Staphylococcus aureus: an experimental study[J]. International journal of infectious diseases, 2008, 12(4): 396-401.
| Cell experiment [1]: | |
Cell lines | THP-1 cells |
Preparation Method | Linezolid (up to 24 h at 1.18mM) on cell viability was assessed by the Trypan Blue exclusion test. |
Reaction Conditions | 1.18mM; 24h |
Applications | Linezolid did not have a toxic effect on uninfected THP-1 cells in the concentration range used in our experiments. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | A partial upper median sternotomy was performed on 70 rats. The animals were divided into seven groups: an uncontaminated control group; an untreated contaminated group; three contaminated groups treated with antibiotics intraperitoneally with either 25 or 50 mg/kg linezolid twice a day, or rifampin 5 mg/kg twice a day; and two contaminated groups that received a combination therapy consisting of 25 or 50 mg/kg linezolid and rifampin 5 mg/kg twice a day. The antibiotic treatment lasted 7 days. |
Dosage form | 25 or 50mg/kg; i.p. |
Applications | The 25-mg/kg dose of linezolid was not effective in reducing the bacterial counts in mediastinum and sternum. Quantitative bacterial cultures of mediastinum and sternum were significantly lower in the groups receiving 50 mg/kg linezolid alone or in combination with rifampin compared with the control. |
References: | |
| Cas No. | 165800-03-3 | SDF | |
| المرادفات | PNU 100766 | ||
| Chemical Name | N-[[(5S)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide | ||
| Canonical SMILES | CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCOCC3)F | ||
| Formula | C16H20FN3O4 | M.Wt | 337.35 |
| الذوبان | ≥ 16.85mg/mL in DMSO, ≥ 9.5 mg/mL in EtOH with ultrasonic, ≥ 2.48 mg/mL in Water with ultrasonic and warming | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9643 mL | 14.8214 mL | 29.6428 mL |
| 5 mM | 592.9 μL | 2.9643 mL | 5.9286 mL |
| 10 mM | 296.4 μL | 1.4821 mL | 2.9643 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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