| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
Ceftibuten (Sch39720) exhibits good efficacy against Proteus, Escherichia coli, Haemophilus influenzae, and Klebsiella species. Quite effective against Serratia species. and Pyogenes streptococcus. Ceftibuten exhibits poor efficacy against Pseudomonas aeruginosa and obligate anaerobic bacteria, and is comparatively ineffective against enterococci and staphylococci. With the exception of Bacteroides fragilis, most organisms that produce beta-lactamases exhibit stability. Ceftibuten has a low level of activity against Campylobacter jejuni (average MIC for 90% of strains = 16.0 μg/ml), but a high level of effectiveness against strains of Enterobacteriaceae (average MIC for 90% of strains = 0.25 μg/ml) [1].
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| ln Vivo |
The biostable beta-lactam antibiotic ceftibuten has been demonstrated to be transported in rat intestinal brush border membrane vesicles by a tiny peptide transport mechanism with a high affinity for the carrier. Transport properties that are reliant on proton gradient and stereoselective [3].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed after oral administration. Cefiboxene is excreted in the urine; 95% of the administered radioactive material is recovered in urine or feces. 0.21 L/kg [Adult Subjects] 0.5 L/kg [Fasting Pediatric Patients] Metabolisms/Metabolites A study of radiolabeled cefiboxene in six healthy adult male volunteers showed that cis-cefiboxene was the major component in plasma and urine. Approximately 10% of cefiboxene is converted to the trans isomer, which has approximately 1/8 the antibacterial potency of the cis isomer. Elimination pathway: Cefbuprofen is excreted in the urine; 95% of the administered radioactive material is recovered in the urine or feces. |
| Toxicity/Toxicokinetics |
Toxicity Summary
Cefobacterium exerts its bactericidal effect by binding to key target proteins in the bacterial cell wall. This binding leads to inhibition of cell wall synthesis. Effects During Pregnancy and Lactation ◉ Overview of Use During Lactation Limited information suggests that cefobacterium concentrations in breast milk are low and are not expected to have adverse effects on breastfed infants. There are reports that cephalosporins occasionally disrupt the infant's gut microbiota, leading to diarrhea or thrush, but these effects have not been fully assessed. Cefobacterium can be used in breastfeeding women. ◉ Effects on Breastfed Infants No relevant published information was found as of the revision date. ◉ Effects on Lactation and Breast Milk No relevant published information was found as of the revision date. ◉ Protein Binding Cefobacterium binds to plasma proteins at a rate of 65%. Protein binding is independent of plasma cefobacterium concentration. |
| References |
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| Additional Infomation |
Ceftibuten is a third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazolyl-4-yl)-4-carboxybut-2-enoyl]amino substituent at position 7 of its cephalosporin skeleton. Ceftibuten is an oral medication, used in dihydrate form to treat urinary tract and respiratory tract infections. It is an antibacterial drug belonging to the cephalosporin and dicarboxylic acid classes. It is commonly used to treat acute bacterial exacerbations of chronic bronchitis (ABECB), acute bacterial otitis media, pharyngitis, and tonsillitis. Ceftibuten is a cephalosporin antibacterial drug. Ceftibuten is a semi-synthetic, β-lactamase-stabilized third-generation cephalosporin with antibacterial activity. Ceftibuten binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of bacterial cell walls. PBPs are enzymes involved in the final stages of bacterial cell wall assembly and in the remodeling of cell walls during growth and division. Inactivation of PBPs interferes with the cross-linking of peptidoglycan chains, which is crucial for the strength and rigidity of bacterial cell walls. This leads to weakening of the bacterial cell wall and cell lysis. Cefbuspirone is a third-generation cephalosporin antibiotic. It is an oral medication. Cefalexin is used to treat acute bacterial exacerbations of chronic bronchitis (ABECB), acute bacterial otitis media, pharyngitis, and tonsillitis. Cephalosporin antibiotics are used to treat a variety of infections, including urinary tract infections and respiratory tract infections. See also: Cefbuspirone dihydrate (active ingredient). Indications: For the treatment of acute bacterial exacerbations of chronic bronchitis (ABECB), acute bacterial otitis media, pharyngitis, and tonsillitis. Mechanism of Action: Cefbuspirone exerts its bactericidal effect by binding to key target proteins in the bacterial cell wall. This binding leads to inhibition of cell wall synthesis.
Pharmacodynamics Cefobacterium is an antibiotic with bactericidal activity. |
| Molecular Formula |
C15H14N4O6S2
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|---|---|
| Molecular Weight |
410.42486
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| Exact Mass |
410.035
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| CAS # |
97519-39-6
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| Related CAS # |
Ceftibuten dihydrate;118081-34-8;Ceftibuten hydrate;1346153-47-6
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| PubChem CID |
5282242
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
966.4±65.0 °C at 760 mmHg
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| Flash Point |
538.3±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.762
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| LogP |
-0.96
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
755
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C1[C@@H](NC(=O)/C(/C2N=C(N)SC=2)=C\CC(=O)O)[C@H]2SCC=C(N12)C(=O)O
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| InChi Key |
UNJFKXSSGBWRBZ-BJCIPQKHSA-N
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| InChi Code |
InChI=1S/C15H14N4O6S2/c16-15-17-7(5-27-15)6(1-2-9(20)21)11(22)18-10-12(23)19-8(14(24)25)3-4-26-13(10)19/h1,3,5,10,13H,2,4H2,(H2,16,17)(H,18,22)(H,20,21)(H,24,25)/b6-1-/t10-,13-/m1/s1
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| Chemical Name |
(6R,7R)-7-[[(Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino]-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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4365 mL | 12.1826 mL | 24.3653 mL | |
| 5 mM | 0.4873 mL | 2.4365 mL | 4.8731 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4365 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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