1. Anti-infection
  2. Antibiotic Bacterial Penicillin-binding protein (PBP)
  3. Cefozopran dihydrochloride

Cefozopran dihydrochloride  (Synonyms: SCE-2787 dihydrochloride)

Cat. No.: HY-W740077
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Cefozopran (SCE-2787) dihydrochloride is a potent antibiotic with broad-spectrum antibacterial activity. Cefozopran dihydrochloride binds PBPs, induces cell wall destruction, cell elongation, filamentation, irregular septa formation, and bactericidal, bacteriolytic activity. Cefozopran dihydrochloride reduces bacterial counts and eradicates bacteria in mouse respiratory, urinary, and thigh muscle infections. Cefozopran dihydrochloride can be used for the research of bacterial infections.

For research use only. We do not sell to patients.

Cefozopran dihydrochloride

Cefozopran dihydrochloride Chemical Structure

CAS No. : 1262200-57-6

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Description

Cefozopran (SCE-2787) dihydrochloride is a potent antibiotic with broad-spectrum antibacterial activity. Cefozopran dihydrochloride binds PBPs, induces cell wall destruction, cell elongation, filamentation, irregular septa formation, and bactericidal, bacteriolytic activity. Cefozopran dihydrochloride reduces bacterial counts and eradicates bacteria in mouse respiratory, urinary, and thigh muscle infections. Cefozopran dihydrochloride can be used for the research of bacterial infections[1][2][3][4].

In Vitro

Cefozopran (20 h) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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 (5-80 mg/kg; s.c.; twice daily; 5 days) dihydrochloride exhibits potent efficacy against acute K. pneumoniae respiratory tract infection in mice[2].
Cefozopran (20-80 mg/kg; s.c.; twice daily; 7 days) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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.

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]
Dosage: 5; 20; 80 mg/kg
Administration: s.c.; twice daily; 5 days
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.
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]
Dosage: 20; 40; 80 mg/kg
Administration: s.c.; twice daily; 7 days
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.
Animal Model: CBA/J mice with urinary tract infection induced by transurethral inoculation of Pseudomonas aeruginosa P9 with urethral clamping for 6 hours[2]
Dosage: 1.56; 6.25; 25; 100 mg/kg
Administration: s.c.; twice daily; 5 days; tarting 3 days after infection
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.
Animal Model: ICR mice with thigh muscle infection induced by injection of Methicillin-sensitive Staphylococcus aureus[2]
Dosage: 0.625; 2.5; 10; 40 mg/kg
Administration: s.c.; single dose at 2, 18, 26 hours post-infection
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.
Animal Model: ICR mice with thigh muscle infection induced by injection of Methicillin-resistant Staphylococcus aureus N133[2]
Dosage: 3.125; 12.5; 50; 200 mg/kg
Administration: s.c.; single dose at 2, 18, 26 hours post-infection
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.
Molecular Weight

588.45

Formula

C19H19Cl2N9O5S2

CAS No.
SMILES

[H][C@@]12N(C([C@@]2([H])NC(/C(C3=NSC(N)=N3)=N/OC)=O)=O)C(C([O-])=O)=C(CS1)C[N+]4=C5C=CC=NN5C=C4.Cl.Cl

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Cefozopran dihydrochloride
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