1. Anti-infection
    Neuronal Signaling
  2. Bacterial
    Antibiotic
    Monoamine Oxidase
  3. Contezolid

Contezolid (Synonyms: MRX-I)

Cat. No.: HY-19915 Purity: 99.37% ee.: 99.28%
Handling Instructions

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).

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

Contezolid Chemical Structure

Contezolid Chemical Structure

CAS No. : 1112968-42-9

Size Price Stock Quantity
5 mg USD 800 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 4200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 6700 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Contezolid:

Top Publications Citing Use of Products

View All Monoamine Oxidase Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[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.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (293.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4490 mL 12.2450 mL 24.4900 mL
5 mM 0.4898 mL 2.4490 mL 4.8980 mL
10 mM 0.2449 mL 1.2245 mL 2.4490 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: ≥ 2.08 mg/mL (5.09 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.37% ee.: 99.28%

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Contezolid
Cat. No.:
HY-19915
Quantity:
MCE Japan Authorized Agent: