Contezolid

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Contezolid (MRX I) 是一种口服活性恶唑烷酮化合物，对革兰氏阳性病原体具有抗菌活性，包括 MRSA、青霉素-PRSP、PISP 和耐万古霉素肠球菌 (VRE)，MIC 为 0.25-4 ug/mL。

Contezolid (MRX I) is an orally active oxazolidinone agent with antibacterial activity Gram-positive pathogens, including MRSA, penicillin-PRSP, PISP, and vancomycin-resistant enterococci (VRE) with MIC of 0.25-4 ug/mL; demonstrates the same or better efficacy than linezolid in both systemic and local infection models against the tested strains.Bacterial Infection Phase 3 Clinical.

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.

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 (P < 0.05). There was no statistical difference between twice daily 50 mg/kg of MRX-I and 25mg/kg (P > 0.05).Animal Model:Rats.Dosage:20, 100, and 200/300 mg/kg/day.Administration:Orally twice daily.Result:No mortality was observed.

MRX I

GPCR/G Protein

Antibacterial

Antibacterial

Infection

Bacterial Infection

1112968-42-9

408.337

C18H15F3N4O4

>98% (HPLC)

In Vitro:?DMSO : 120 mg/mL (293.88 mM)

O=C1CCN(C2=C(F)C=C(N3C(O[C@@H](CNC4=NOC=C4)C3)=O)C(F)=C2F)C=C1

1-{2,3,6-trifluoro-4-[(5S)-5-{[(1,2-oxazol-3-yl)amino]methyl}-2-oxo-1,3-oxazolidin-3-yl]phenyl}-2,3-dihydropyridin-4(1H)-one

(-20℃)

With Ice Pack

≥ 2 years