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Tebipenem Pivoxil

Name: Tebipenem Pivoxil
Brand: Selleck Chemicals
SKU: S2159

Synonyms: L-084, ME1211,TBPM-PI,LJC 11036

Catalog No.S2159 Purity: 99.65%

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

Tebipenem Pivoxil Chemical Structure

CAS: 161715-24-8

Purity & Quality Control

Batch: Purity: 99.65%

99.65

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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
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
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04919954	Completed	Diabetes\|Wound Infection\|ABSSSI\|Healthy Volunteers	Hartford Hospital\|Spero Therapeutics	July 1 2021	Phase 1
NCT04625855	Completed	Healthy Volunteers	Spero Therapeutics\|Covance	September 30 2020	Phase 1
NCT04376554	Completed	Healthy Volunteers	Spero Therapeutics\|Iqvia Pty Ltd	February 10 2020	Phase 1
NCT04178577	Completed	Renal Impairment	Spero Therapeutics	December 6 2019	Phase 1

References

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Chemical lnformation & Solubility

Molecular Weight	497.63	Formula	C₂₂H₃₁N₃O₆S₂
CAS No.	161715-24-8	SDF	Download Tebipenem Pivoxil SDF
Smiles	CC1C2C(C(=O)N2C(=C1SC3CN(C3)C4=NCCS4)C(=O)OCOC(=O)C(C)(C)C)C(C)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 99 mg/mL ( (198.94 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 87 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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