Tebipenem Pivoxil Chemical Structure
Molecular Weight: 497.63 Tebipenem Pivoxil is a novel oral carbapenem antibiotic with an IC50 of 100 μg/ml for human CYP isoforms
Tebipenem pivoxil(L-084) is a novel oral carbapenem antibiotic with an IC50 of 100 µg/ml for human CYP isoforms. In mouse, rat, dog and monkey, TBPM-PI were absorbed quickly, and the bioavailability was (71.4, 59.1, 34.8 and 44.9%, respectively. There was no other tissue than the kidney, in which TBPM was highly distributed and remained for a long time. In addition, low penetration to the central nervous system was confirmed. The penetration ratio of TBPM to ELF, that is the ratio of ELF concentration to plasma concentration of TBPM, was 21.8 +/- 14.7%.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
|Body Surface Area (m2)||0.6||0.5||0.24||0.15||0.05||0.025||0.02||0.007|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×||mouse Km(3)||= 11.2 mg/kg|
|Molecular Weight (MW)||497.63|
|Storage||3 years -20℃Powder|
|6 months-80℃in solvent (DMSO, water, etc.)|
|Solubility (25°C) *||In vitro||DMSO||99 mg/mL (198.94 mM)|
|Water||<1 mg/mL (|
|Ethanol||87 mg/mL (174.82 mM)|
|Chemical Name||(4R,5S,6S)-pivaloyloxymethyl 3-(1-(4,5-dihydrothiazol-2-yl)azetidin-3-ylthio)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylate|
|Stock Solution (1ml DMSO)||1mM||10mM||20mM||30mM|
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