Omadacycline hydrochloride是新开发的,用于治疗社区获得性细菌感染的氨基甲基四环素抗生素。对大肠杆菌的ED50值为2.02 mg/kg。
Description | Omadacycline hydrochloride is novel, aminomethyl tetracycline antibiotic being developed for the treatment of community-acquired bacterial infections. The ED50 for Escherichia coli is 2.02 mg/kg. | ||||||||||||||||
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IC50 & Target | ED50: 2.02 mg/kg (Escherichia coli), 0.30-1.74 mg/kg (Staphylococcus aureus)[1] | ||||||||||||||||
In Vitro | The omadacycline MIC90s for MRSA, VRE, and beta-hemolytic streptococci are 1.0 μg/mL, 0.25 μg/mL, and 0.5 μg/mL, respectively, and the omadacycline MIC90s for PRSP and H. influenzae are 0.25 μg/ml and 2.0 μg/mL, respectively. Omadacycline is active against organisms demonstrating the two major mechanisms of resistance, ribosomal protection and active tetracycline efflux[1]. Omadacycline inhibits protein synthesis while having no significant effect on RNA, DNA and peptidoglycan synthesis. Further, omadacycline binds to the tetracycline binding site on the 30S subunit of the bacterial ribosome with enhanced binding similar to tigecycline based on additional molecular interactions[2]. | ||||||||||||||||
In Vivo | In vivo efficacy of omadacycline is demonstrated using an intraperitoneal infection model in mice. A single intravenous dose of omadacycline exhibits efficacy against Streptococcus pneumoniae, Escherichia coli, and Staphylococcus aureus, including tet (M) and tet (K) efflux-containing strains and MRSA strains. The 50% effective doses (ED50s) for Streptococcus pneumoniae obtained ranged from 0.45 mg/kg to 3.39 mg/kg, the ED50s for Staphylococcus aureus obtained ranges from 0.30 mg/kg to 1.74 mg/kg, and the ED50 for Escherichia coli is 2.02 mg/kg[1]. | ||||||||||||||||
Clinical Trial | | ||||||||||||||||
Solvent & Solubility | In Vitro: H2O : ≥ 50 mg/mL (84.30 mM) * "≥" means soluble, but saturation unknown. Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References | |
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