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Tebipenem Pivoxil 161715-24-8

Product Description

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Tebipenem Pivoxil

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


Biological Activity


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)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

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
rat Km(6)




Chemical Information




Molecular Weight (MW) 497.63
Formula

C22H31N3O6S2

CAS No. 161715-24-8

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms L-084, ME1211



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
Mass(mg) 0.49763 4.9763 9.9526 14.9289


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