2. Anti-infection
    Neuronal Signaling
  3. Bacterial
    Antibiotic
    Monoamine Oxidase
  4. Contezolid acefosamil sodium

Contezolid acefosamil sodium  (Synonyms: MRX-4 sodium)

Cat. No.: HY-19915B Purity: 99.38%
COA Handling Instructions

Contezolid acefosamil sodium (MRX-4), 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 acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI).

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

Contezolid acefosamil sodium Chemical Structure

Contezolid acefosamil sodium Chemical Structure

CAS No. : 1807365-35-0

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Contezolid acefosamil sodium:

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MAO-A MAO-B

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Contezolid acefosamil sodium (MRX-4), 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 acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI)[1][2].

IC50 & Target

Oxazolidinone

 

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

552.33

Appearance

Solid

Formula

C20H17F3N4NaO8P
CAS No.
SMILES

FC(C(F)=C1N(C=C2)CCC2=O)=C(N(C(O3)=O)C[[email protected]@H]3CN(C4=NOC=C4)[P](OC(C)=O)(O[Na])=O)C=C1F
Shipping

Shipping with dry ice.
Storage

-80°C, stored under nitrogen
Solvent & Solubility
In Vitro: 

DMSO : 180 mg/mL (325.89 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8105 mL 9.0526 mL 18.1051 mL
5 mM 0.3621 mL 1.8105 mL 3.6210 mL
10 mM 0.1811 mL 0.9053 mL 1.8105 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 4.5 mg/mL (8.15 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 4.5 mg/mL (8.15 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 4.5 mg/mL (8.15 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Contezolid acefosamil1807365-35-0MRX-4MRX4MRX 4BacterialAntibioticMonoamine OxidaseMAOG+bacteriamonoamineoxidasecSSTIMRSAInhibitorinhibitorinhibit

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