替​比​培​南​匹​酯 T6231

Product Introduction
Bioactivity


英文名: Tebipenem Pivoxil

描述: Tebipenem Pivoxil (Orapenem) 是一种碳青霉烯类新型口服抗生素。

体外活性: 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]

体内活性: 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 81 mg/mL (162.8 mM)
DMSO : 92 mg/mL (184.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: Antibiotic | broad antibacterial spectrum | L 084 | penicillin-binding protein | inhibit | L-084 | Inhibitor | orally active | ME-1211 | Haemophilus influenza | L084 | Bacterial | Tebipenem Pivoxil | Erythromycin-resistant Streptococcus pneumonia | Streptococcus pneumonia | ME 1211

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相关库: Drug Repurposing Compound Library | Antibiotics Library | ReFRAME Related Library | FDA-Approved & Pharmacopeia Drug Library | Clinical Compound Library | Human Metabolite Library | Pediatric Drug Library | NO PAINS Compound Library | Bioactive Compound Library | Anti-Infection Compound Library

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