| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Penicillin-binding proteins (PBPs): PBP 3, 1A, and 1Bs.
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|---|---|
| ln Vitro |
Cefteram exhibits broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria; it is particularly active against Streptococcus pyogenes (ten times more active than cefaclor) and Gram-negative pathogens causing meningitis and gonorrhea; MIC values vary by organism.
|
| ln Vivo |
In pediatric patients and animal infection models, cefteram pivoxil demonstrates clinical efficacy against various bacterial infections; in a pediatric study, 30 cases showed excellent clinical response, and all 28 identified bacteria were eradicated post-treatment.
|
| Enzyme Assay |
Binding to penicillin-binding proteins (PBPs) is assessed by competitive binding assays using bacterial membrane preparations from target pathogens; membranes are incubated with radiolabeled penicillin (e.g., 3H-benzylpenicillin) and serial dilutions of cefteram; bound radioactivity is measured after filtration.
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| Cell Assay |
Cefteram pivoxil is first dissolved in DMSO and then diluted in appropriate culture media; minimal inhibitory concentrations (MICs) are determined by broth microdilution or agar dilution methods according to CLSI guidelines; bacterial cultures are incubated with serial two-fold dilutions of the compound for 18-24 hours; MIC is defined as the lowest concentration with no visible growth.
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| Animal Protocol |
Mouse models of bacterial infection are used: mice are infected intraperitoneally with a lethal dose of target bacteria (e.g., S. aureus, S. pyogenes, E. coli); cefteram pivoxil is administered orally as a suspension at various doses; survival rates and bacterial counts in organs are measured; ED50 values are calculated.
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| ADME/Pharmacokinetics |
PK: After oral administration, cefteram pivoxil is rapidly absorbed and hydrolyzed by esterases to active cefteram; Cmax is reached within 2-3 hours; plasma half-life is approximately 1-1.5 hours; primarily excreted unchanged in urine; food intake can affect bioavailability (urinary recovery: 33% in non-fasted vs 18% in fasted subjects).
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| Toxicity/Toxicokinetics |
Toxicity: Cefteram pivoxil is generally well-tolerated in clinical use; common side effects include gastrointestinal disturbances (diarrhea, nausea) and mild hypersensitivity reactions; as a cephalosporin, cross-allergy with penicillins may occur; no significant hepatotoxicity or nephrotoxicity reported at therapeutic doses.
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| References | |
| Additional Infomation |
Ceftaram pivoxil is a neopentyloxymethyl ester, belonging to the cephalosporin, oxime, tetrazolium, and 1,3-thiazole classes. Ceftaram pivoxil is a prodrug of cefadroxil, a semi-synthetic, broad-spectrum third-generation cephalosporin with antibacterial activity. After oral administration of cefadroxil pivoxil, the ester bond breaks, releasing the active ingredient cefadroxil.
Cefteram pivoxil (Ro-19-5248, T-2588) is a third-generation oral cephalosporin approved for clinical use in Japan and certain other countries; it is indicated for the treatment of bacterial infections including pharyngitis, tonsillitis, bronchitis, pneumonia, urinary tract infections, and otitis media; it is not approved by FDA (US) or EMA (Europe) as of this knowledge cutoff. |
| Molecular Formula |
C22H27N9O7S2
|
|---|---|
| Molecular Weight |
593.63588
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| Exact Mass |
593.147
|
| CAS # |
82547-81-7
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| PubChem CID |
5362114
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| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.66 g/cm3
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| Melting Point |
125-128ºC
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| Index of Refraction |
1.744
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| LogP |
0.724
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
40
|
| Complexity |
1100
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C(C1=C(CN2N=NC(C)=N2)CS[C@@H]2[C@@H](C(N12)=O)NC(=O)/C(/C1=CSC(N)=N1)=N\OC)(=O)OCOC(=O)C(C)(C)C
|
| InChi Key |
UIYAXIPXULMHAI-JLGRZTKVSA-N
|
| InChi Code |
InChI=1S/C22H27N9O7S2/c1-10-26-29-30(27-10)6-11-7-39-18-14(25-16(32)13(28-36-5)12-8-40-21(23)24-12)17(33)31(18)15(11)19(34)37-9-38-20(35)22(2,3)4/h8,14,18H,6-7,9H2,1-5H3,(H2,23,24)(H,25,32)/b28-13-/t14-,18-/m1/s1
|
| Chemical Name |
2,2-dimethylpropanoyloxymethyl (6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-[(5-methyltetrazol-2-yl)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
|
| 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 | 1.6845 mL | 8.4226 mL | 16.8452 mL | |
| 5 mM | 0.3369 mL | 1.6845 mL | 3.3690 mL | |
| 10 mM | 0.1685 mL | 0.8423 mL | 1.6845 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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