| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Cefditoren targets penicillin-binding proteins (PBPs) in the bacterial cell wall. By binding to these proteins, it inhibits bacterial cell wall synthesis, leading to cell lysis and death. Cefditoren is a broad-spectrum antibiotic commonly used against bacteria responsible for community-acquired pneumonia and pharyngitis.
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| ln Vitro |
Cefditoren (sodium) exhibits good action against Moraxella catarrhalis, Haemophilus influenzae, Haemophilus parainfluenzae, Staphylococcus aureus, and Streptococcus pneumoniae [1]. Microorganism MIC50 (mg/L) MIC90 (mg/L) Susceptible (%) Gram-positive bacteria Streptococcus pneumoniae (untyped)a 0.015-0.25 0.12-1 PS ≤0.008-0.03 0.015-0.25 99-100 PI 0.06-0.5 0.25- 0.5 94-100 PR 0.25-1 0.5-2 7-100 Streptococcus pyogenes ≤0.008-0.03 0.015-0.03 100 Staphylococcus aureus (MS) 0.12-0.5 0.5-1 50-100 Gram Negative bacteria Haemophilus ≤0.008-≤0.03 0.01 5 -0.13 influenza bacilli (untyped)b β-lactamase+ ≤0.008-0.03 0.015-0.06 100 β-lactamase- ≤0.008-0.03 0.015-0.06 100 Haemophilus parainfluenzae ≤0.03 0.06 Moraxella 0.03-0.5 0.25-1 96 Catarrhalis (untyped)b β-lactamase+ ≤0.03-0.25 0.12-0.5 100 β-lactamase- ≤0.008 -0.03 0.015-0.06 100 an Includes PS, PI and PR strains. b Contains both positive and negative strains of β-lactamase. MIC50/90 is the average minimum inhibitory concentration needed to stop the development of 50% or 90% of strains; MS stands for methicillin susceptibility, PI for moderate penicillin sensitivity, PR for penicillin resistance, and PS for penicillin susceptibility.
In vitro, Cefditoren demonstrates antibacterial activity against a broad range of Gram-positive and Gram-negative bacteria. It has been used in comparative studies to ascertain the effectiveness of newly synthesized antibiotics and in in vitro testing of antibiotic resistance in bacteria. Minimum inhibitory concentrations (MICs) for susceptible organisms are in the low microgram per milliliter range. |
| ln Vivo |
Mouse pharmacokinetics [1]:Tlast (h) 6.25 53.0 0.9 30.4 6 12.5 168.4 1.1 64.1 8 25 232.5 0.9 101.3 8 50 290.6 1.1 124.4 8 Cefditoren (mg/kg) C0 (μg/ml) t1/2 (h) AUClast (μg× h/ml)
In vivo, Cefditoren is effective in treating respiratory and skin infections caused by susceptible bacteria. It is used clinically for the treatment of community-acquired pneumonia, acute exacerbations of chronic bronchitis, streptococcal pharyngitis/tonsillitis, and uncomplicated skin and skin structure infections. |
| Enzyme Assay |
In vitro susceptibility testing for cephalosporins typically uses broth microdilution or agar dilution methods according to CLSI guidelines. Bacterial cultures are prepared at a standardized inoculum and incubated with varying concentrations of Cefditoren. Minimum inhibitory concentrations (MICs) are determined as the lowest concentration that inhibits visible bacterial growth after 18-24 hours of incubation.
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| Cell Assay |
In vitro cellular assays for antibiotics typically involve bacterial cell culture. Bacteria are grown in appropriate media and treated with varying concentrations of Cefditoren. Bacterial growth is monitored by measuring optical density (OD600) over time to generate growth curves. Time-kill assays are performed to determine whether the compound is bactericidal or bacteriostatic.
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| Animal Protocol |
In vivo animal studies for antibacterial efficacy typically use mouse or rat models of infection. Animals are infected with a pathogenic bacterial strain and treated with Cefditoren at various doses via oral or parenteral administration. Bacterial load in target organs (e.g., lungs, blood) is determined by CFU counting. Survival is monitored as an endpoint.
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| ADME/Pharmacokinetics |
Cefditoren sodium is administered orally for the treatment of bacterial infections. It is well-absorbed following oral administration and distributes to various tissues, including the respiratory tract. The compound is metabolized in the liver, and its metabolites are excreted via the kidneys and bile. Cefditoren has a favorable PK profile for the treatment of respiratory infections.
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| Toxicity/Toxicokinetics |
Cefditoren is generally well-tolerated at therapeutic doses. Common side effects may include gastrointestinal disturbances, diarrhea, nausea, and headache. Hypersensitivity reactions, including rash and anaphylaxis, may occur in penicillin-allergic patients. As with other cephalosporins, caution should be exercised in patients with a history of penicillin allergy.
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| References |
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| Additional Infomation |
Cefditoren sodium (ME-1206) is a β-lactam cephalosporin antibiotic that inhibits bacterial cell wall synthesis by targeting penicillin-binding proteins. It is used for the treatment of respiratory tract infections, including community-acquired pneumonia and acute exacerbations of chronic bronchitis, as well as skin infections. The compound is available for research and clinical use.
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| Molecular Formula |
C19H18N6O5S3.NA
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|---|---|
| Molecular Weight |
529.56822
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| Exact Mass |
528.032
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| CAS # |
104146-53-4
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| Related CAS # |
Cefditoren (Pivoxil);117467-28-4;Cefditoren-13C,d3
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| PubChem CID |
9589470
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| Appearance |
White to light yellow solid powder
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| LogP |
0.868
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
928
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=C(SC=N1)/C=C/C2=C(N3[C@@H]([C@@H](C3=O)NC(=O)/C(=N/OC)/C4=CSC(=N4)N)SC2)C(=O)O.[Na+]
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| InChi Key |
VFUMWBZIKOREOO-ZSCWKNKWSA-N
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| InChi Code |
InChI=1S/C19H18N6O5S3.Na/c1-8-11(33-7-21-8)4-3-9-5-31-17-13(16(27)25(17)14(9)18(28)29)23-15(26)12(24-30-2)10-6-32-19(20)22-10;/h3-4,6-7,13,17H,5H2,1-2H3,(H2,20,22)(H,23,26)(H,28,29);/q;+1/b4-3+,24-12+;/t13-,17-;/m1./s1
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| Chemical Name |
sodium;(6R,7R)-7-[[(2E)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-[(E)-2-(4-methyl-1,3-thiazol-5-yl)ethenyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~189.19 mM)
DMSO : ~31.25 mg/mL (~59.12 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8883 mL | 9.4416 mL | 18.8832 mL | |
| 5 mM | 0.3777 mL | 1.8883 mL | 3.7766 mL | |
| 10 mM | 0.1888 mL | 0.9442 mL | 1.8883 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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