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

Cefozopran hydrochloride  (Synonyms: SCE-2787 hydrochloride)

Cat. No.: HY-B0771A Purity: 95.03%
Handling Instructions Technical Support

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.

Cefozopran hydrochloride

Cefozopran hydrochloride Chemical Structure

CAS No. : 113981-44-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Cefozopran hydrochloride:

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  • Purity & Documentation

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Description

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[1][2][3][4].

IC50 & Target

β-lactam

 

In Vitro

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.

In Vivo

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

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

551.99

Formula

C19H18ClN9O5S2

CAS No.
Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8116 mL 9.0581 mL 18.1163 mL
5 mM 0.3623 mL 1.8116 mL 3.6233 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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
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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 hydrochloride
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