Methicillin (sodium salt)
(Synonyms: 甲氧西林钠; Meticillin sodium) 目录号 : GC10917
甲氧西林Methicillin是一种窄谱β -内酰胺类抗生素，通过抑制青霉素结合蛋白(PBP)起作用。
Cas No.:132-92-3
Sample solution is provided at 25 µL, 10mM.
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Methicillin is a narrow-spectrum beta-lactam antibiotic that acts by inhibiting penicillin-binding proteins (PBP). Methicillin has a good effect on penicillinase producing S. aureus. Methicillin is not absorbed orally and must be administered by injection. It can be used to treat septicemia, endocarditis, pneumonia, meningitis, brain abscess, pericarditis, urinary tract infection, skin soft tissue infection, osteomyelitis, pseudomembranous enteritis. Methicillin can also be used to screen for resistant strains [1-3].
Methicillin (20 μg/mL; 24 h) results in a rapid decrease in CFU of S. aureus[4]. Methicillin (0-100 μg/mL; 24 h) has a high killing effect on CI-G S. aureus. Strain [5].
Methicillin (intramuscular administration; 40 mg/kg every 6 h; 5 days) reduced mortality in in S. aureus.-infected rabbits[4]. Methicillin (9 μg/ml; 4days; 0.5 ml/day) and a bismuth metal-organic framework (Bi-MOF) can synergistically enhance the therapeutic effect and inhibit the recurrence of infection in the tolerant S. aureus-induced murine subcutaneous infection model [6].
References:
[1]. Katsipis G, Pantazaki AA. Serrapeptase impairs biofilm, wall, and phospho-homeostasis of resistant and susceptible Staphylococcus aureus. Appl Microbiol Biotechnol. 2023 Feb;107(4):1373-1389. doi: 10.1007/s00253-022-12356-5. Epub 2023 Jan 13. PMID: 36635396; PMCID: PMC9898353.
[2]. Khoshnood S, Heidary M,et,al. A review on mechanism of action, resistance, synergism, and clinical implications of mupirocin against Staphylococcus aureus. Biomed Pharmacother. 2019 Jan;109:1809-1818. doi: 10.1016/j.biopha.2018.10.131. Epub 2018 Nov 26. PMID: 30551435.
[3]. Xie X, Tong X, et,al. Use of mouse primary epidermal organoids for USA300 infection modeling and drug screening. Cell Death Dis. 2023 Jan 11;14(1):15. doi: 10.1038/s41419-022-05525-x. PMID: 36631452; PMCID: PMC9833019.
[4]. Carrizosa J, Santoro J, et,al. Treatment of experimental Staphylococcus aureus endocarditis: comparison of cephalothin, cefazolin, and methicillin. Antimicrob Agents Chemother. 1978 Jan;13(1):74-7. doi: 10.1128/AAC.13.1.74. PMID: 626493; PMCID: PMC352187.
[5]. Banerjee S, Sionov RV et,al. Anandamide alters the membrane properties, halts the cell division and prevents drug efflux in multidrug resistant Staphylococcus aureus. Sci Rep. 2021 Apr 22;11(1):8690. doi: 10.1038/s41598-021-88099-6. PMID: 33888802; PMCID: PMC8062478.
[6]. Yuan, Kai et al. “Multi-roles of nanoscale bismuth metal-organic frameworks: Infectious photoacoustic probe and inhibitor of antibiotics tolerant bacteria via targeting endogenous H2S.” Nano Today (2022): n. pag.
甲氧西林Methicillin是一种窄谱β -内酰胺类抗生素，通过抑制青霉素结合蛋白(PBP)起作用。甲氧西林对产青霉素酶的金黄色葡萄球菌有良好的抑制作用。甲氧西林不能口服吸收，必须注射给药。可用于治疗败血症、心内膜炎、肺炎、脑膜炎、脑脓肿、心包炎、尿路感染、皮肤软组织感染、骨髓炎、假膜性肠炎等。甲氧西林也可用于筛选甲氧西林耐药菌株[1-3]。
甲氧西林(20 μg/mL; 24 h)可迅速降低金黄色葡萄球菌的CFU[4]。甲氧西林(0-100 μg/mL; 24 h)对CI-G金黄色葡萄球菌有较高的杀伤效果[5]。
甲氧西林(intramuscular administration; 40 mg/kg every 6 h; 5 days)降低了感染金黄色葡萄球菌的兔子的死亡率[4]。甲氧西林(9 μg/ml; 4days; 0.5 ml/day)和Bi-MOF在耐药金黄色葡萄球菌诱导的小鼠皮下感染模型中可协同增强治疗效果并抑制感染复发[6]。
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Cell experiment [1]: |
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Cell lines |
S. aureus |
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Preparation method |
The rate at which the S. aureus was killed was studied in flasks with heart infusion broth (HIB) containing methicillin. The inoculum in HIB was added to each flask and incubated at 37℃. The final concentrations of antibiotics were 20 μg/ml, and of S. aureus were 3 × 106/ml. Samples were removed from the flasks at the start of the experiment and at 2, 4, 6, and 24 h. Each sample was serially diluted in 10-fold steps in HIB, and 0.1 ml of each dilution and 1 ml of undiluted sample were plated on the surfaces of blood agar plates. After incubation at 37℃ for 48 h the numbers of colonies on the plates were counted and the colony-forming units (CFU) in the flasks were calculated. |
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Reaction Conditions |
20 μg/mL; 24 h |
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Applications |
Methicillin results in a rapid decrease in CFU of S. aureus. |
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Animal experiment [1]: |
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Animal models |
S. aureus.-infected rabbits |
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Preparation method |
Rabbits were anesthetized and cannulated. One day later, each rabbit was inoculated by ear vein with 1 ml of HIB containing 2 × 106 S. aureus. Inoculated control animals were left untreated. In treatment groups, antibiotic therapy was initiated 18 h after infection; the regimens was：methicillin, 40 mg/kg every 6 h. |
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Dosage form |
Intramuscular administration; 40 mg/kg every 6 h; 5 days |
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Applications |
Methicillin reduced mortality in in S. aureus.-infected rabbits. |
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References: [1]. Carrizosa J, Santoro J, et,al. Treatment of experimental Staphylococcus aureus endocarditis: comparison of cephalothin, cefazolin, and methicillin. Antimicrob Agents Chemother. 1978 Jan;13(1):74-7. doi: 10.1128/AAC.13.1.74. PMID: 626493; PMCID: PMC352187. |
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| Cas No. | 132-92-3 | SDF | |
| 别名 | 甲氧西林钠; Meticillin sodium | ||
| 化学名 | (2S,5R,6R)-6-[(2,6-dimethoxybenzoyl)amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, monosodium salt | ||
| Canonical SMILES | O=C(N[C@@H]1C(N2[C@]1([H])SC(C)(C)[C@@H]2C([O-])=O)=O)C3=C(OC)C=CC=C3OC.[Na+] | ||
| 分子式 | C17H19N2O6S • Na | 分子量 | 402.4 |
| 溶解度 | ≥ 14.4mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4851 mL | 12.4254 mL | 24.8509 mL |
| 5 mM | 0.497 mL | 2.4851 mL | 4.9702 mL |
| 10 mM | 0.2485 mL | 1.2425 mL | 2.4851 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet