产品
编 号：F627523
分子式：C18H15F3N4O4
分子量：408.33
分子式：C18H15F3N4O4
分子量：408.33
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 1112968-42-9
产品详情
生物活性：
Contezolid (MRX-I), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI).
体内研究：
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.Animal Model:BALB/c mice infected intranasally with M. tuberculosis Erdman.
Dosage:100, 50 (twice), 25 (twice) mg/kg.
Administration:Gavage, once or twice daily, five days per week for four weeks.
Result:Significantly reduced the CFU recovered from the lungs compared to the early and late control mice (P < 0.05).Twice daily MRX-I at 50mg/kg and 25 mg/kg were significantly better than the late control mice (P < 0.05). Once daily MRX-I at 100 mg/kg was significantly better than twice daily 50 mg/kg and 25 mg/kg (P0.05).
Animal Model:Rats.
Dosage:20, 100, and 200/300 mg/kg/day.
Administration:Orally twice daily.
Result:No mortality was observed.
体外研究：
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.
Contezolid (MRX-I), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI).
体内研究：
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.Animal Model:BALB/c mice infected intranasally with M. tuberculosis Erdman.
Dosage:100, 50 (twice), 25 (twice) mg/kg.
Administration:Gavage, once or twice daily, five days per week for four weeks.
Result:Significantly reduced the CFU recovered from the lungs compared to the early and late control mice (P < 0.05).Twice daily MRX-I at 50mg/kg and 25 mg/kg were significantly better than the late control mice (P < 0.05). Once daily MRX-I at 100 mg/kg was significantly better than twice daily 50 mg/kg and 25 mg/kg (P0.05).
Animal Model:Rats.
Dosage:20, 100, and 200/300 mg/kg/day.
Administration:Orally twice daily.
Result:No mortality was observed.
体外研究：
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.
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