Tebipenem Pivoxil

SKU: orb1223262

Description

Tebipenem pivoxil, also known as ME1211; SPR994 and TBM-PI, is a novel oral carbapenem antibiotic. TBM-PI is a promising antibiotic for the treatment of acute otitis media. Tebipenem pivoxil displays an excellent antibacterial activity against a variety of pathogenic bacteria in vitro. Importantly, tebipenem pivoxil significantly protects the sepsis mice challenged with various pathogenic bacteria, which may provide a potential approach to treating bacterial sepsis in clinic.(In Vitro):Tebipenem pivoxil (0-128 μg/mL; 18–24 h) displays excellent antibacterial activity against a variety of pathogenic bacteria.(In Vivo):Tebipenem pivoxil (L084) (0-4.00 g/kg; p.o.; once) shows minimal lethal dosage (MLD) of 4.00 g/kg and the maximum tolerance dosage (MTD) of 3.40 g/kg in mice.Tebipenem pivoxil (50 and 100 mg/kg; p.o.; once) significantly protects the sepsis mice challenged with various pathogenic bacteria.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 161715-24-8
• MW: 497.63
• Purity: >98% (HPLC)
• Formula: C₂₂H₃₁N₃O₆S₂
• SMILES: C[C@@H]1[C@@H]2[C@H](C(=O)N2C(=C1SC1CN(C1)C1=NCCS1)C(=O)OCOC(=O)C(C)(C)C)[C@@H](C)O
• Target: PAK
• Solubility: DMSO : ≥ 150 mg/mL; 301.43 mM

Bioactivity

• In Vivo:
  Tebipenem pivoxil (L084) (0-4.00 g/kg; p.o. ; once) shows minimal lethal dosage (MLD) of 4.00 g/kg and the maximum tolerance dosage (MTD) of 3.40 g/kg in mice. Tebipenem pivoxil (50 and 100 mg/kg; p.o. ; once) significantly protects the sepsis mice challenged with various pathogenic bacteria. Animal model: KM mice weighing 18–22 g. Dosage: 2.89, 3.40 and 4.00 g/kg. Administration: Oral administration (tablet), once. Result: Within the 14-day observation period, only one mouse was dead in the maximum oral dosage (4.00 g/kg). The minimal lethal dosage (MLD) was 4.00 g/kg and the maximum tolerance dosage (MTD) in the mice was 3.40 g/kg. Showed dose-dependent liver and kidney damage. Animal model: ICR mice, sepsis mouse models. Dosage: 50 and 100 mg/kg. Administration: Oral administration (tablet), once. Result: Significantly increased the survival number of the sepsis mice within a 168 h observation period.
• In Vitro:
  Tebipenem pivoxil (0-128 μg/mL; 18-24 h) displays excellent antibacterial activity against a variety of pathogenic bacteria. Cell Viability Assay Cell line: Gram-positive and Gram-negative bacteria. Concentration: 0-128 μg/mL. Incubation time: 18-24 h. Result: Showed inhibition with MIC50s below 64 μg/mL against tested Gram-positive and Gram-negative bacteria.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ME1211 | SPR994 | TBM-PI | Tebipenem pivoxil

Quick Database Links

Gene Symbol

PAK