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| Size | Price | Stock |
|---|---|---|
| 250mg | $650 | Check With Us |
| 500mg | $900 | Check With Us |
| 1g | $1350 | Check With Us |
: Cat #: V2512 CAS #: 161715-24-8 Purity ≥ 98%
Description: Tebipenem pivoxil (also known as L-084, ME1211) is an orally bioavailable, broad spectrum antibiotic of the carbapenem class structurally, it is use to treat otolaryngologic and respiratory infections. It was developed as a replacement drug to combat bacteria that had acquired antibiotic resistance to commonly used antibiotics. Tebipenem is formulated as the ester tebipenem pivoxil due to the better absorption and improved bioavailability of this form. It has performed well in clinical trials for ear infection and looks likely to be further developed in future. 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.
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| Molecular Weight (MW) | 497.63 |
|---|---|
| Molecular Formula | C22H31N3O6S2 |
| CAS No. | 161715-24-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 99 mg/mL (198.9 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 87 mg/mL (174.8 mM) | |
| SMILES Code | O=C1[C@H]([C@H](O)C)[C@]2([H])[C@@H](C)C(SC3CN(C4=NCCS4)C3)=C(C(OCOC(C(C)(C)C)=O)=O)N12 |
| Synonyms | L-084, L 084, L084, ME1211; ME-1211; ME 1211; SPR994; SPR-994; SPR 994; TBM-PI |
| Protocol | In Vitro | In vitro activity: 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. 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. 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. Tebipenem 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. 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. | |
| Animal model | KM mice weighing 18–22 g | |
| Dosages | 2.89, 3.40 and 4.00 g/kg | |
| Administration | Oral administration (tablet), once |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.0095 mL | 10.0476 mL | 20.0953 mL | 40.1905 mL |
| 5mM | 0.4019 mL | 2.0095 mL | 4.0191 mL | 8.0381 mL |
| 10mM | 0.2010 mL | 1.0048 mL | 2.0095 mL | 4.0191 mL |
| 20mM | 0.1005 mL | 0.5024 mL | 1.0048 mL | 2.0095 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.