Tebipenem pivoxil (L-084, ME1211) is an oral carbapenem antibiotic, use to treat otolaryngologic and respiratory infections.
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Bacterial penicillin-binding protein inhibitor
Product Description
Information
Tebipenem pivoxil (L-084, ME1211) is an oral carbapenem antibiotic, use to treat otolaryngologic and respiratory infections. In vitro
Tebipenem Pivoxil has high\xa0intestinal apical membrane permeability due to plural intestinal transport routes, including the uptake transporters such as OATP1A2 and OATP2B1 as well as simple diffusion. Tebipenem Pivoxil is quickly converted to tebipenem\xa0(TBPM), an active form of\xa0Tebipenem Pivoxil. Tebipenem Pivoxil are absorbed quickly, and the bioavailability is 71.4%, 59.1%, 34.8% and 44.9%, respectively, in mouse, rat, dog and monkey. Tebipenem shows the strongest bactericidal activity as early as 2 h after exposure at two times the MIC. Tebipenem shows higher affinities for PBP 1A and PBP 2B, high-molecular-weight enzymes, and for PBP 3, a low-molecular-weight enzyme, than for PBP 2X.\xa0 Tebipenem\xa0has a potent\xa0activity\xa0against\xa0Neisseria gonorrhoeae; its\xa0activity\xa0is comparable to it of cefixime that has most potent activity among oral antibiotics.
In vivo
Tebipenem Pivoxil results in survival rate of 83%, compared with 25% survival for Amoxicillin and 0% survival for controls in animal model of\xa0otitis\xa0media. Tebipenem\xa0exhibits\xa0slow\xa0tight-binding inhibition at low micromolar concentrations versus the chromogenic\xa0substrate\xa0nitrocefin.\xa0Tebipenem\xa0acyl-enzyme complex remains stable for greater than 90 min and exists as mixture of the covalently bound drug and the bound retro-aldol cleavage product. Cell Data
