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Tebipenem Pivoxil (L084) Carbapenem Antibiotic

Cat.No.S2159

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

Batch: Purity: 99.65%
99.65

Solubility

In vitro
Batch:

DMSO : 99 mg/mL (198.94 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 87 mg/mL

Water : Insoluble

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In vivo
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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.

Chemical Information, Storage & Stability

Molecular Weight 497.63 Formula

C22H31N3O6S2

Storage (From the date of receipt)
CAS No. 161715-24-8 Download SDF Storage of Stock Solutions

Synonyms L-084, ME1211,TBPM-PI,LJC 11036 SMILES CC1C2C(C(=O)N2C(=C1SC3CN(C3)C4=NCCS4)C(=O)OCOC(=O)C(C)(C)C)C(C)O

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Mechanism of Action

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. This compound is quickly converted to tebipenem (TBPM), an active form. It is 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. It 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.  This chemical has a potent activity against Neisseria gonorrhoeae; its activity is 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 otitis media. This compound exhibits slow tight-binding inhibition at low micromolar concentrations versus the chromogenic substrate nitrocefin. It 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.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/19673353/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17055132/
  • [6] https://pubmed.ncbi.nlm.nih.gov/24846409/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-05-20)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06727136 COMPLETED
Healthy Participants
Spero Therapeutics
2024-11-20 PHASE1
NCT05121974 COMPLETED
Shigellosis
International Centre for Diarrhoeal Disease Research, Bangladesh
2022-08-18 PHASE2
NCT06059846 COMPLETED
Urinary Tract Infection; Acute Pyelonephritis
Spero Therapeutics
2023-12-21 PHASE3
NCT05856747 COMPLETED
Healthy Volunteers
Spero Therapeutics
2023-05-04 PHASE1
NCT04919954 COMPLETED
Diabetes; Wound Infection; ABSSSI; Healthy Volunteers
Hartford Hospital
2021-07-01 PHASE1
NCT04919954 Completed
Diabetes|Wound Infection|ABSSSI|Healthy Volunteers
Hartford Hospital|Spero Therapeutics
2021-07-01 Phase 1

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