Cefozopran hydrochloride
Based on 1 Customer Validation
Cefozopran (SCE-2787) hydrochloride is a potent antibiotic with broad-spectrum antibacterial activity. Cefozopran hydrochloride binds PBPs, induces cell wall destruction, cell elongation, filamentation, irregular septa formation, and bactericidal, bacteriolytic activity. Cefozopran hydrochloride reduces bacterial counts and eradicates bacteria in mouse respiratory, urinary, and thigh muscle infections. Cefozopran hydrochloride can be used for the research of bacterial infections.
For research use only. We do not sell to patients.
- Purity: 95.03%
- CAS No.: 113981-44-5
- Formula: C19H18ClN9O5S2
- Molecular Weight:551.99
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Storage:
-20°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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Biological Activity
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β-lactam |
Cefozopran (20 h) hydrochloride potently inhibits growth of Streptococcus pyogenes, Staphylococcus aureus, Enterococcus faecalis, and shows particularly strong activity against Streptococcus species, Enterobacteriaceae (except Proteus vulgaris), and Methicillin (HY-121544)-susceptible staphylococci[4].
Cefozopran (20 h) hydrochloride inhibits growth of various laboratory aerobic bacterial strains, with MIC values ranging from 0.1 μg/mL to 50 μg/mL, and shows limited activity against tested anaerobic strains[4].
Cefozopran (20 h) hydrochloride is highly active against Ceftazidime (HY-B0593)-resistant Citrobacter freundii (MIC90 = 3.13 μg/mL) and Enterobacter cloacae (MIC90 = 12.5 μg/mL), but shows cross-resistance with Ceftazidime against Ceftazidime-resistant Pseudomonas aeruginosa (MIC90 >100 μg/mL)[4].
Cefozopran (200 μM) hydrochloride is highly resistant to hydrolysis by most common β-lactamases, including Bush group 1, 2a, 2b, and 2c enzymes, but is hydrolyzed to varying degrees by Bush group 2b', 2d, and 2e enzymes[4].
Cefozopran hydrochloride has low affinity for all tested β-lactamases, with Km/Ki values all >100 μM, indicating minimal interaction with these enzymes[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cefozopran (20-80 mg/kg; s.c.; twice daily; 7 days) hydrochloride effectively eradicates chronic K. pneumoniae respiratory tract infection in mice[2].
Cefozopran (1.56-100 mg/kg; s.c.; twice daily; 5 days; tarting 3 days after
infection) hydrochloride demonstrates potent efficacy against P. aeruginosa urinary tract infection in mice[2].
Cefozopran (0.625-200 mg/kg; s.c.; dose at 2, 18, 26 hours post-infection) hydrochloride shows strong efficacy against MSSA thigh muscle abscess infection in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (4-week-old, male) with acute respiratory tract infection induced by aerosol exposure to Klebsiella pneumoniae DT-S for 40 minutes[2]
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Dosage:5; 20; 80 mg/kg
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Administration:s.c.; twice daily; 5 days
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Result:Showed 0/10 survival rate and 0/10 lung sterilization rate at 5 mg/kg.
Showed 8/10 survival rate and 2/10 lung sterilization rate at 20 mg/kg.
Showed 10/10 survival rate and 10/10 lung sterilization rate at 80 mg/kg.
Achieved an SD50 of 13.8 mg/kg and a CD50 of 29.0 mg/kg.
Had an MIC of 0.05 μg/mL against Klebsiella pneumoniae DT-S.
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Animal Model:CBA/J mice (5-week-old, female) with chronic respiratory tract infection induced by aerosol exposure to Klebsiella pneumoniae 27 for 60 minutes[2]
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Dosage:20; 40; 80 mg/kg
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Administration:s.c.; twice daily; 7 days
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Result:Showed 1/12 lung sterilization rate at 20 mg/kg.
Showed 0/11 lung sterilization rate at 40 mg/kg.
Showed 12/12 lung sterilization rate at 80 mg/kg.
Achieved a CD50 of 55.2 mg/kg.
Had an MIC of 0.05 μg/mL against Klebsiella pneumoniae 27.
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Animal Model:CBA/J mice with urinary tract infection induced by transurethral inoculation of Pseudomonas aeruginosa P9 with urethral clamping for 6 hours[2]
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Dosage:1.56; 6.25; 25; 100 mg/kg
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Administration:s.c.; twice daily; 5 days; tarting 3 days after infection
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Result:Showed 3/15 kidney sterilization rate at 1.56 mg/kg.
Showed 7/15 kidney sterilization rate at 6.25 mg/kg.
Showed 11/15 kidney sterilization rate at 25 mg/kg.
Showed 12/15 kidney sterilization rate at 100 mg/kg.
Achieved a CD50 of 8.78 mg/kg.
Had an MIC of 0.78 μg/mL against Pseudomonas aeruginosa P9.
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Animal Model:ICR mice with thigh muscle infection induced by injection of Methicillin-sensitive Staphylococcus aureus[2]
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Dosage:0.625; 2.5; 10; 40 mg/kg
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Administration:s.c.; single dose at 2, 18, 26 hours post-infection
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Result:Showed a mean bacterial count of 6.14 log CFU and an effective rate of 2/8 at 0.625 mg/kg.
Showed a mean bacterial count of 5.38 log CFU and an effective rate of 3/8 at 2.5 mg/kg.
Showed a mean bacterial count of 4.77 log CFU and an effective rate of 6/8 at 10 mg/kg.
Showed a mean bacterial count of 4.59 log CFU and an effective rate of 8/8 at 40 mg/kg.
Achieved an ED50 of 2.87 mg/kg.
Had an MIC of 0.39 μg/mL against methicillin-sensitive Staphylococcus aureus.
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Animal Model:ICR mice with thigh muscle infection induced by injection of Methicillin-resistant Staphylococcus aureus N133[2]
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Dosage:3.125; 12.5; 50; 200 mg/kg
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Administration:s.c.; single dose at 2, 18, 26 hours post-infection
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Result:Showed a mean bacterial count of 7.63 log CFU and an effective rate of 0/8 at 3.125 mg/kg.
Showed a mean bacterial count of 7.55 log CFU and an effective rate of 0/8 at 12.5 mg/kg.
Showed a mean bacterial count of 6.54 log CFU and an effective rate of 2/8 at 50 mg/kg.
Showed a mean bacterial count of 4.82 log CFU and an effective rate of 7/8 at 200 mg/kg.
Achieved an ED50 of 79.8 mg/kg.
Had an MIC of 50 μg/mL against methicillin-resistant Staphylococcus aureus N133.
Chemical Information
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CAS No. 113981-44-5
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Appearance Solid
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Molecular Weight 551.99
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Formula C19H18ClN9O5S2
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Color White to light yellow
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SMILES
[H]Cl.[O-]C(C(N1[C@@]2([H])[C@H](NC(/C(C3=NSC(N)=N3)=N\OC)=O)C1=O)=C(CS2)C[N+]4=C(C=CC=N5)N5C=C4)=O
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Synonyms
SCE-2787 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (181.16 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 (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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (4.53 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 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: ≥ 2.5 mg/mL (4.53 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.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Nakao M, et al. Antibacterial properties of SCE-2787, a new cephem antibiotic. J Antimicrob Chemother. 1992;29(5):509-518. [Content Brief]
[2]. Iizawa Y, et al. Therapeutic effect of cefozopran (SCE-2787), a new parenteral cephalosporin, against experimental infections in mice. Antimicrob Agents Chemother. 1993;37(1):100-105. [Content Brief]
[3]. Klein O, et al. In vitro activity of SCE-2787, a new cephalosporin with potent activity against Pseudomonas aeruginosa and members of the family Enterobacteriaceae. Antimicrob Agents Chemother. 1994;38(12):2896-2901. [Content Brief]
[4]. Iwahi T, et al. In vitro and in vivo activities of SCE-2787, a new parenteral cephalosporin with a broad antibacterial spectrum. Antimicrob Agents Chemother. 1992;36(7):1358-1366. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8116 mL | 9.0581 mL | 18.1163 mL | 45.2907 mL |
| 5 mM | 0.3623 mL | 1.8116 mL | 3.6233 mL | 9.0581 mL | |
| 10 mM | 0.1812 mL | 0.9058 mL | 1.8116 mL | 4.5291 mL | |
| 15 mM | 0.1208 mL | 0.6039 mL | 1.2078 mL | 3.0194 mL | |
| 20 mM | 0.0906 mL | 0.4529 mL | 0.9058 mL | 2.2645 mL | |
| 25 mM | 0.0725 mL | 0.3623 mL | 0.7247 mL | 1.8116 mL | |
| 30 mM | 0.0604 mL | 0.3019 mL | 0.6039 mL | 1.5097 mL | |
| 40 mM | 0.0453 mL | 0.2265 mL | 0.4529 mL | 1.1323 mL | |
| 50 mM | 0.0362 mL | 0.1812 mL | 0.3623 mL | 0.9058 mL | |
| 60 mM | 0.0302 mL | 0.1510 mL | 0.3019 mL | 0.7548 mL | |
| 80 mM | 0.0226 mL | 0.1132 mL | 0.2265 mL | 0.5661 mL | |
| 100 mM | 0.0181 mL | 0.0906 mL | 0.1812 mL | 0.4529 mL |
Cefozopran hydrochloride Related Classifications
HY-B0771A Related Classifications
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- Cefozopran
- 113981-44-5
- SCE-2787
- SCE2787
- SCE 2787
- Antibiotic
- Bacterial
- Penicillin-binding protein (PBP)
- β-lactamases
- Escherichia coli PBP 3
- methicillin-resistant Staphylococcus aureus
- Staphylococcus aureus PBPs 1-2
- Citrobacter freundii
- Klebsiella pneumoniae
- Enterococcus faecalis
- Enterobacter cloacae
- Streptococcus pyogenes
- Pseudomonas aeruginosa PBPs 1-3
- Inhibitor
- inhibitor
- inhibit