Cefozopran
Cefozopran (SCE-2787) is a potent antibiotic with broad-spectrum antibacterial activity. Cefozopran binds PBPs, induces cell wall destruction, cell elongation, filamentation, irregular septa formation, and bactericidal, bacteriolytic activity. Cefozopran reduces bacterial counts and eradicates bacteria in mouse respiratory, urinary, and thigh muscle infections. Cefozopran can be used for the research of bacterial infections.
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- CAS. Nr.: 113359-04-9
- Formel: C19H17N9O5S2
- Molecular Weight:515.53
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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- Reinheit & Dokumentation
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Biologische Aktivität
Beschreibung
IC50 & Target
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β-lactam |
In Vitro
Cefozopran (20 h) 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) 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) 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) 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 dihydrochloride 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.
In Vivo
Cefozopran (20-80 mg/kg; s.c.; twice daily; 7 days) 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) 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) 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. Nr. 113359-04-9
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Molecular Weight 515.53
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Formel C19H17N9O5S2
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SMILES
[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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Cefozopran Related Classifications
HY-B0771 Related Classifications
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Keywords
- Cefozopran
- 113359-04-9
- 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