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Tebipenem

泰比培南
Catalog No.
B4864
广谱口服抗生素
组合的产品项目
规格价格库存 数量
5mg
¥ 1,436.00
现货
10mg
¥ 2,418.00
现货
50mg
¥ 6,481.00
现货

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A

背景

Tebipenem is an orally available carbapenem antibiotic. Tebipenem is active against a panel of clinical isolates from a variety of bacterial species (MIC50s ≤ 0.0039 ~ 8 µg/ml), including methicillin-resistant strains of Staphylococcus aureus (S. aureus) and Staphylococcus epidermidis (S. epidermidis), as well as penicillin-resistant Streptococcus pneumoniae (S. pneumonia). Tebipenem also inhibits β-lactamase in a time- and concentration-dependent manner. Tebipenem pivoxil, a derivative of tebipenem, has been under development as the first orally available carbapenem antibiotic for the treatment of respiratory and otolaryngological infections caused by drug-resistant S. pneumonia in pediatric patients.

References:

1. Hazra S, Xu H, Blanchard JS. Tebipenem, a new carbapenem antibiotic, is a slow substrate that inhibits the β-lactamase from Mycobacterium tuberculosis. Biochemistry, 2014, 53(22): 3671-3678.

2. Fujimoto K, Takemoto K, Hatano K, et al. Novel carbapenem antibiotics for parenteral and oral applications: in vitro and in vivo activities of 2-aryl carbapenems and their pharmacokinetics in laboratory animals. Antimicrobial Agents and Chemotherapy, 2013, 57(2): 697-707.

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt383.49
Cas No.161715-21-5
FormulaC16H21N3O4S2
Solubilityinsoluble in EtOH; ≥19.15 mg/mL in H2O with gentle warming; ≥24.9 mg/mL in DMSO
Chemical Name(4R,5S,6S)-3-[1-(4,5-dihydro-1,3-thiazol-2-yl)azetidin-3-yl]sulfanyl-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
SDFDownload SDF
Canonical SMILESCC1C2C(C(=O)N2C(=C1SC3CN(C3)C4=NCCS4)C(=O)O)C(C)O
运输条件 蓝冰运输或根据您的需求运输。
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试验操作

Animal experiment:[2]

Animal models

A mouse model of penicillin-resistant S. pneumoniae infection

Dosage form

0.32 ~ 3.2 mg/kg

Administered intravenously thrice daily 1 day and 2 days after infection

Applications

Tebipenem dose-dependently decreased the number of colony forming units (CFUs) in the lungs of infected mice.

Note

The technical data provided above is for reference only.

References:

1. Hazra S, Xu H, Blanchard JS. Tebipenem, a new carbapenem antibiotic, is a slow substrate that inhibits the β-lactamase from Mycobacterium tuberculosis. Biochemistry, 2014, 53(22): 3671-3678.

2. Fujimoto K, Takemoto K, Hatano K, et al. Novel carbapenem antibiotics for parenteral and oral applications: in vitro and in vivo activities of 2-aryl carbapenems and their pharmacokinetics in laboratory animals. Antimicrobial Agents and Chemotherapy, 2013, 57(2): 697-707.

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