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Tebipenem Pivoxil (L084) Carbapenem Antibiotic

Name: Tebipenem Pivoxil (L084)
Brand: Selleck Chemicals
SKU: S2159
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S2159

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

Chemical Structure

Molecular Weight: 497.63

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.65%

99.65

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Chemical Information, Storage & Stability

Molecular Weight	497.63	Formula	C₂₂H₃₁N₃O₆S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	161715-24-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.900mg/ml (9.85mM)	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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.400mg/ml (4.82mM)	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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

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. ^[1] 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. ^[2] 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. ^[3] 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. ^[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] 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. ^[6]
References	[1] https://pubmed.ncbi.nlm.nih.gov/20735088/ [2] https://pubmed.ncbi.nlm.nih.gov/19882982/ [3] https://pubmed.ncbi.nlm.nih.gov/15728880/ [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 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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