Linezolid
(Synonyms: 利奈唑胺; PNU-100766) 目录号 : GC11221
利奈唑胺（Linezolid; PNU-100766）是一种具有口服活性的恶唑烷酮类抗生素，对多种革兰氏阳性菌具有抑制活性，包括耐甲氧西林金黄色葡萄球菌（MRSA）、糖肽中间体金黄色葡萄球菌（GISA）、耐万古霉素肠球菌（VRE）和耐青霉素肺炎链球菌。
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.
利奈唑胺（Linezolid; PNU-100766）是一种具有口服活性的恶唑烷酮类抗生素，对多种革兰氏阳性菌具有抑制活性，包括耐甲氧西林金黄色葡萄球菌（MRSA）、糖肽中间体金黄色葡萄球菌（GISA）、耐万古霉素肠球菌（VRE）和耐青霉素肺炎链球菌[1]。Linezolid是一种50S核糖体亚基特异性抑制剂，作用机制是在50S核糖体亚基上结合抑制蛋白质合成的起始步骤[2]。Linezolid对葡萄球菌（Staphylococcus aureus）蛋白质合成的IC50为0.3μg/ml，对50S亚基形成的IC50为0.6μg/ml[3]。Linezolid适用于治疗皮肤感染、细菌性肺炎和菌血症并发的感染[4]。
在体外，Linezolid（1.18mM）处理被金黄色葡萄球菌（ATCC 25923和E19977）感染的THP-1细胞24h，对细胞活力没有影响，但是对细胞内及细胞外的菌株有显著抑制作用[5]。
在体内，Linezolid（50mg/kg）通过腹腔注射治疗MRSA纵隔炎的大鼠7天，显著减少了纵隔和胸骨中的细菌计数[6]。
| 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 | |
| 别名 | 利奈唑胺; PNU-100766 | ||
| 化学名 | 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 | ||
| 分子式 | C16H20FN3O4 | 分子量 | 337.35 |
| 溶解度 | ≥ 16.85mg/mL in DMSO, ≥ 9.5 mg/mL in EtOH with ultrasonic, ≥ 2.48 mg/mL in Water with ultrasonic and warming | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9643 mL | 14.8214 mL | 29.6428 mL |
| 5 mM | 0.5929 mL | 2.9643 mL | 5.9286 mL |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9643 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet