Ceftolozane (sulfate)
Based on 2 publication(s) in Google Scholar
Ceftolozane (CXA-101) sulfate is an antipseudomonal cephalosporin. Ceftolozane binds to P. aeruginosa essential PBPs (1b, 1c, 2 and 3) with high affinity. Ceftolozane inhibits cell wall synthesis by binding the PBPs. Ceftolozane sulfate inhibits P. aeruginosa and Enterobacteriaceae.
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- 純度: 99.69%
- CAS 番号: 936111-69-2
- 分子式: C23H32N12O12S3
- 分子量:764.77
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Ceftolozane sulfate
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生物活性
MIC: 0.5 μg/mL (P. aeruginosa PAO1)[1]
Ceftolozane sulfate shows antibacterial activity against fully AmpC-derepressed P. aeruginosa, with MIC of 4 mg/L[4].
Ceftolozane sulfate (≤0.12->64 μg/mL) shows antipseudomonal activity, including against carbapenem-resistant and MDR isolates, with MICs of >8 μg/mL for 11 carbapenem-resistant P. aeruginosa isolates (4.7%)[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ceftolozane (180 mg/kg, s.c., every 8 h, 48 h) sulfate reduces bacterial load and improves early pulmonary inflammatory response without impairing 48 h post-infection homeostasis in a mice model of Pseudomonas aeruginosa acute pneumonia[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Neutropenic murine thigh infection model[6]
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Dosage:400, 800 mg/kg
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Administration:Subcutaneous injection (s.c.), every 6 h
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Result:Reduced ESBL-producing Enterobacteriaceae.
Showed that ceftolozane with tazobactam at a 2:1 ratio were significantly different than animals treated with ceftolozane alone.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 936111-69-2
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性状 Solid
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分子量 764.77
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分子式 C23H32N12O12S3
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Color White to off-white
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SMILES
O=S(O)(O)=O.CN1[N+](CC(CS[C@]2([H])[C@@H]3NC(/C(C4=NSC(N)=N4)=N\OC(C)(C(O)=O)C)=O)=C(C([O-])=O)N2C3=O)=CC(NC(NCCN)=O)=C1N
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別名
CXA-101; FR264205
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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PLoS Pathog
Differential contribution of PBP occupancy and efflux on the effectiveness of β-lactams at their target site in clinical isolates of Neisseria gonorrhoeae. [Abstract]2024 Dec 31;20(12):e1012783. PMID: 39739989 -
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
溶剤 & 溶解度
DMSO : 50 mg/mL (65.38 mM; ultrasonic and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 10 mg/mL (13.08 mM; Need ultrasonic)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (279 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Moyá B, et al. Affinity of the new cephalosporin CXA-101 to penicillin-binding proteins of Pseudomonas aeruginosa. Antimicrob Agents Chemother. 2010 Sep;54(9):3933-7. [Content Brief]
[2]. Moya B, et al. Activity of a new cephalosporin, CXA-101 (FR264205), against beta-lactam-resistant Pseudomonas aeruginosa mutants selected in vitro and after antipseudomonal treatment of intensive care unit patients. Antimicrob Agents Chemother. 2010 Mar;54(3):1213-7. [Content Brief]
[3]. Kostoulias X, et al. Ceftolozane/tazobactam disrupts Pseudomonas aeruginosa biofilms under static and dynamic conditions. J Antimicrob Chemother. 2025 Feb 3;80(2):372-380. [Content Brief]
[4]. Livermore DM, et al. Activity of cephalosporin CXA-101 (FR264205) against Pseudomonas aeruginosa and Burkholderia cepacia group strains and isolates. Int J Antimicrob Agents. 2009 Nov;34(5):402-6. [Content Brief]
[5]. Juan C, et al. Activity of a new antipseudomonal cephalosporin, CXA-101 (FR264205), against carbapenem-resistant and multidrug-resistant Pseudomonas aeruginosa clinical strains. Antimicrob Agents Chemother. 2010 Feb;54(2):846-51. [Content Brief]
[6]. Craig WA, et al. In vivo activities of ceftolozane, a new cephalosporin, with and without tazobactam against Pseudomonas aeruginosa and Enterobacteriaceae, including strains with extended-spectrum β-lactamases, in the thighs of neutropenic mice. Antimicrob Agents Chemother. 2013 Apr;57(4):1577-82. [Content Brief]
[7]. Jacqueline C, et al. Efficacy of ceftolozane in a murine model of Pseudomonas aeruginosa acute pneumonia: in vivo antimicrobial activity and impact on host inflammatory response. J Antimicrob Chemother. 2013 Jan;68(1):177-83. [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 (sealed storage, away from moisture). 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 | 1.3076 mL | 6.5379 mL | 13.0758 mL | 32.6896 mL |
| 5 mM | 0.2615 mL | 1.3076 mL | 2.6152 mL | 6.5379 mL | |
| 10 mM | 0.1308 mL | 0.6538 mL | 1.3076 mL | 3.2690 mL | |
| DMSO | 15 mM | 0.0872 mL | 0.4359 mL | 0.8717 mL | 2.1793 mL |
| 20 mM | 0.0654 mL | 0.3269 mL | 0.6538 mL | 1.6345 mL | |
| 25 mM | 0.0523 mL | 0.2615 mL | 0.5230 mL | 1.3076 mL | |
| 30 mM | 0.0436 mL | 0.2179 mL | 0.4359 mL | 1.0897 mL | |
| 40 mM | 0.0327 mL | 0.1634 mL | 0.3269 mL | 0.8172 mL | |
| 50 mM | 0.0262 mL | 0.1308 mL | 0.2615 mL | 0.6538 mL | |
| 60 mM | 0.0218 mL | 0.1090 mL | 0.2179 mL | 0.5448 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.
Ceftolozane sulfate 関連分類
HY-19806A 関連分類
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