メシリナム
Based on 4 publication(s) in Google Scholar
Mecillinam (Amdinocillin) is a β-lactam Antibiotic. Mecillinam inhibits PBP2. Mecillinam exhibits activity against Gram-negative Enterobacteriaceae, and NDM-/OXA-producing E. coli and K. pneumoniae, and can eradicate catheter/bladder mucosa biofilms and clear planktonic bacteria in urine. Mecillinam acts synergistically with β-lactams and Avibactam (HY-14879), enhancing the activity of β-lactams against E. coli in vitro/in vivo. Mecillinam can be used in research on catheter-associated bacteriuria, chlamydial infection and peritonitis/sepsis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 32887-01-7
- 分子式: C15H23N3O3S
- 分子量:325.43
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[6]|
β-lactam |
体外実験
Mecillinam (0.4-100 μg/mL; 18 h) inhibits a significant proportion of Gram-negative isolates by the agar dilution method, with 75% of Escherichia coli and 62% of Enterobacter inhibited at 6.3 μg/mL[2].
Mecillinam (0.009-10 mg/L; 18 h) inhibits E. coli O54 with an MIC of 10 mg/L and produces complete growth inhibition when used in combination at 0.156 mg/L (FIC 0.016), with a total FIC of 0.046[4].
Mecillinam (0.0625-32 mg/L; 30 min) binds PBP2 with an IC50 of 0.3 mg/L in the E. coli MG1655 PBP competition assay, and Avibactam (HY-14879) does not alter the PBP binding affinity of Mecillinam[5].
Mecillinam (4 mg/L) combined with 1 mg/L Avibactam effectively kills K. pneumoniae isolates KP2, KP5, KP6, KP7, KP8, and ATCC 13883[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Mecillinam (30 mg/kg alone; 2-8 mg/kg in combination with ampicillin; subcutaneous injection; single injection) is ineffective against normal mice with E. coli thigh infection, but low doses strongly enhance the antibacterial activity of Ampicillin (HY-B0522)[4].
Mecillinam (30 mg/kg alone; 2-8 mg/kg in combination with Ampicillin; subcutaneous injection; single injection) is ineffective against Escherichia coli thigh infection in irradiated granulocytopenic mice, but low doses still enhance the antibacterial activity of Ampicillin[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:New Zealand white (male)[1]
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Dosage:50, 100, 200, or 400 mg/kg body weight each day
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Administration:intravenous; four divided doses each day; 72 h
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Result:At sacrifice, log10 cfu of E. coli/mL or cm2 in urethral catheter were NG for 400 mg/kg, 2.02 for 200 mg/kg (2/6), 0.97 for 100 mg/kg (2/5), and 2.53 for 50 mg/kg (2/5).
At 400 mg/kg, at 48 h four of five rabbits had completely eliminated bacteria from urine; at 72 h all rabbits had sterile catheter urine, and urine, catheter, and bladder wall samples were free of detectable bacteria.
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Animal Model:Swiss-type (SPF, male, 20-25 g)[4]
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Dosage:30 mg/kg (alone); 2 mg/kg (with ampicillin); 4 mg/kg (with ampicillin); 8 mg/kg (with ampicillin)
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Administration:subcutaneous; single injection
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Result:At 30 mg/kg alone, did not produce an antibacterial effect in normal mice.
In combination with ampicillin, produced a strong potentiating effect.
The lowest dose examined in combination was 2 mg/kg.
Potency ratios of the combinations relative to ampicillin alone, plotted against dose in Fig. 5a, increased with dose (2, 4, and 8 mg/kg).
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 32887-01-7
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性状 Solid
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分子量 325.43
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分子式 C15H23N3O3S
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Color White to off-white
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SMILES
O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2/N=C/N3CCCCCC3)N1C2=O)O
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別名
Mecillinam; Amdinocillin; FL 1060
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (4)
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Journal Impact Factor
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Most Recent
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J Antimicrob Chemother
Unravelling the triad of penicillin-binding proteins, β-lactamase activity, and mRNA dynamics in Pseudomonas aeruginosa AmpC induction. [Abstract]2025 Nov 5:dkaf408. PMID: 41206063 -
Microbiol Spectr
Penicillin-Binding Protein Occupancy Dataset for 18 β-Lactams and 4 β-Lactamase Inhibitors in Neisseria gonorrhoeae. [Abstract]2023 Jun 15;11(3):e0069223. PMID: 37093051 -
Microbiol Spectr
PBP Target Profiling by β-Lactam and β-Lactamase Inhibitors in Intact Pseudomonas aeruginosa: Effects of the Intrinsic and Acquired Resistance Determinants on the Periplasmic Drug Availability. [Abstract]2023 Feb 14;11(1):e0303822. PMID: 36475840 -
J Glob Antimicrob Resist
Susceptibility of multidrug-resistant Escherichia coli and Klebsiella pneumoniae to oral antibiotics in Australia. [Abstract]2025 Aug 8:44:435-441. PMID: 40784378
溶剤 & 溶解度
体外:
H2O : 100 mg/mL (307.29 mM; Need ultrasonic)
DMSO : 100 mg/mL (307.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6.25 mg/mL (19.21 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 6.25 mg/mL (19.21 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (307.29 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (284 KB)
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SDS (396 KB)
- English - EN (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Olson ME, et al. Amdinocillin treatment of catheter-associated bacteriuria in rabbits. The Journal of infectious diseases. 1989 Jun;159(6):1065-72. [Content Brief]
[2]. Neu HC, et al. Mecillinam, a novel penicillanic acid derivative with unusual activity against gram-negative bacteria. Antimicrobial agents and chemotherapy. 1976 May;9(5):793-9. [Content Brief]
[5]. List KK, et al. Synergy between Mecillinam and Ceftazidime/Avibactam or Avibactam against Multi-Drug-Resistant Carbapenemase-Producing Escherichia coli and Klebsiella pneumoniae. Antibiotics (Basel). 2022 Sep 20;11(10):1280. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.0729 mL | 15.3643 mL | 30.7286 mL | 76.8214 mL |
| 5 mM | 0.6146 mL | 3.0729 mL | 6.1457 mL | 15.3643 mL | |
| 10 mM | 0.3073 mL | 1.5364 mL | 3.0729 mL | 7.6821 mL | |
| 15 mM | 0.2049 mL | 1.0243 mL | 2.0486 mL | 5.1214 mL | |
| 20 mM | 0.1536 mL | 0.7682 mL | 1.5364 mL | 3.8411 mL | |
| 25 mM | 0.1229 mL | 0.6146 mL | 1.2291 mL | 3.0729 mL | |
| 30 mM | 0.1024 mL | 0.5121 mL | 1.0243 mL | 2.5607 mL | |
| 40 mM | 0.0768 mL | 0.3841 mL | 0.7682 mL | 1.9205 mL | |
| 50 mM | 0.0615 mL | 0.3073 mL | 0.6146 mL | 1.5364 mL | |
| 60 mM | 0.0512 mL | 0.2561 mL | 0.5121 mL | 1.2804 mL | |
| 80 mM | 0.0384 mL | 0.1921 mL | 0.3841 mL | 0.9603 mL | |
| 100 mM | 0.0307 mL | 0.1536 mL | 0.3073 mL | 0.7682 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Mecillinam 関連分類
HY-A0269 関連分類
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