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CAS No. : 1807365-35-0
MCE 国际站:Contezolid acefosamil sodium
产品活性:Contezolid acefosamil sodium (MRX-4) 是一种新型的恶唑烷酮,用于耐药革兰氏阳性菌引起的皮肤组织感染并发症 (cSSTI) 的抗生素。Contezolid acefosamil sodium (MRX-4) 可显著降低骨髓移植和单胺氧化酶抑制。
研究领域:Anti-infection | Neuronal Signaling
作用靶点:Bacterial | Antibiotic | Monoamine Oxidase
In Vitro: Contezolid (MRX-I) is highly potent against all Grampositive clinical isolates of staphylococci, streptococci, and enterococci, including MDR organisms such as MRSA, methicilline-resistant Streptococcus epidermidis (MRSE), penicillin-resistant Streptococci (PRSP), and VRE.
In Vivo: Oral absorption of Contezolid (MRX-I) occurrs rapidly in mouse, rat, and dog, with peak plasma concentrations observed at 0.5−2.6 h postdose. In mouse, rat, and dog, respectively, PK parameters are determined as follows: dose-normalized Cmax/dose was 524, 1065, and 259 ng/mL/(mg/kg); dose-normalized AUC0−t/dose was 1654, 3703, and 1664 ng•h/mL/(mg/kg); T1/2 is 1, 1.5, and 3 h; and the oral bioavailability is 69%, 109%, and 37%.
Contezolid (MRX-I) exhibits no obvious toxicity.
Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to the untreated early and late controls.
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