| Name | Tebipenem Pivoxil |
| Description | Tebipenem Pivoxil (Orapenem) , an orally activity carbapenem antibiotic, is utilized in treating 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 81 mg/mL (162.77 mM), Sonication is recommended.
DMSO : 92 mg/mL (184.88 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (10.05 mM), Sonication is recommended.
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| Keywords | Tebipenem Pivoxil | Streptococcus pneumonia | penicillin-binding protein | orally active | ME-1211 | ME 1211 | L-084 | L084 | L 084 | Inhibitor | inhibit | Haemophilus influenza | Erythromycin-resistant Streptococcus pneumonia | broad antibacterial spectrum | Bacterial | Antibiotic |
| Inhibitors Related | Neomycin sulfate | Adipic dihydrazide | Levulinic acid | D(+)-Raffinose pentahydrate | Sulfamethoxazole sodium | Terbinafine hydrochloride | Doxycycline | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate | Sodium bicarbonate | BES |
| Related Compound Libraries | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Antibiotics Library | Drug Repurposing Compound Library | Beta-Lactam Compound Library | Anti-Bacterial Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Preclinical Compound Library | Anti-Infection Compound Library | Human Metabolite Library |
United States
