Tebipenem Pivoxil

Catalog No.S2159 Batch:S215902

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Technical Data

Formula

C22H31N3O6S2
Molecular Weight 497.63 CAS No. 161715-24-8
Solubility (25°C)* In vitro DMSO 99 mg/mL (198.94 mM)
Ethanol 87 mg/mL (174.82 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
2.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 48 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.9mg/ml Taking the 1 mL working solution as an example, add 50 μL of 98 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Tebipenem pivoxil (L-084, ME1211,TBPM-PI,LJC 11036) is an oral carbapenem antibiotic, use to treat otolaryngologic and respiratory infections.
In vitro

Tebipenem Pivoxil has high intestinal apical membrane permeability due to plural intestinal transport routes, including the uptake transporters such as OATP1A2 and OATP2B1 as well as simple diffusion. [1] Tebipenem Pivoxil is quickly converted to tebipenem (TBPM), an active form of Tebipenem 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. [2] 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. [3] Tebipenem has a potent activity against Neisseria gonorrhoeae; its activity is comparable to it of cefixime that has most potent activity among oral antibiotics. [4]
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 otitis media. [5] Tebipenem exhibits slow tight-binding inhibition at low micromolar concentrations versus the chromogenic substrate nitrocefin. Tebipenem acyl-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. [6]

Protocol (from reference)

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.