1. Anti-infection
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    Antibiotic
    Monoamine Oxidase
  3. Contezolid

Contezolid (Synonyms: MRX-I)

Cat. No.: HY-19915
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Contezolid (MRX-I), a new and oraly 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).

For research use only. We do not sell to patients.

Contezolid Chemical Structure

Contezolid Chemical Structure

CAS No. : 1112968-42-9

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Description

Contezolid (MRX-I), a new and oraly 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)[1][2].

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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%[2].
Contezolid (MRX-I) exhibits no obvious toxicity[2].
Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to the untreated early and late controls[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice infected intranasally with M. tuberculosis Erdman[3].
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[2].
Dosage: 20, 100, and 200/300 mg/kg/day.
Administration: Orally twice daily.
Result: No mortality was observed.
Clinical Trial
Molecular Weight

408.33

Formula

C₁₈H₁₅F₃N₄O₄

CAS No.

1112968-42-9

SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ContezolidMRX-IBacterialAntibioticMonoamine OxidaseMAOtuberculosisGram-positiveMRASMAOIInhibitorinhibitorinhibit

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Contezolid
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