Contezolid
Based on 4 publication(s) in Google Scholar
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).
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- Pureza: 99.21%
- No. CAS: 1112968-42-9
- Fòrmula: C18H15F3N4O4
- Peso molecular:408.33
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Almacenamiento:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Contezolid
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Actividad biológica
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Oxazolidinone |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice infected intranasally with M. tuberculosis Erdman[3].
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Dosage:100, 50 (twice), 25 (twice) mg/kg.
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Administration:Gavage, once or twice daily, five days per week for four weeks.
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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).
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Animal Model:Rats[2].
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Dosage:20, 100, and 200/300 mg/kg/day.
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Administration:Orally twice daily.
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Result:No mortality was observed.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1112968-42-9
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Appearance Solid
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Peso molecular 408.33
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Fòrmula C18H15F3N4O4
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Color White to light yellow
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SMILES
O=C1CCN(C2=C(F)C=C(N3C(O[C@@H](CNC4=NOC=C4)C3)=O)C(F)=C2F)C=C1
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Synonyms
MRX-I
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
Publications (4)
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Journal Impact Factor
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Most Recent
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Front Microbiol
Antibacterial and anti-biofilm activity of radezolid against Staphylococcus aureus clinical isolates from China. [Abstract]2023 Apr 26:14:1131178. PMID: 37180277 -
Antimicrob Agents Chemother
Side-by-Side Profiling of Oxazolidinones to Estimate the Therapeutic Window against Mycobacterial Infections. [Abstract]2023 Apr 18;67(4):e0165522. PMID: 36920191 -
ACS Omega
In Vitro Activity of Sulfamethoxazole-Trimethoprim, Amikacin, Oxazolidinones, Fluoroquinolones and Fidaxomicin against Isolates of Nocardia. [Abstract]2025 Oct 27;10(44):52289-52295. PMID: 41244472 -
BMC Microbiol
Contezolid and polymyxin B nonapeptide combination reveals antibacterial synergy against multidrug-resistant Acinetobacter baumannii strains. [Abstract]2026 May 29. PMID: 42216156
Solvente y solubilidad
DMSO : 120 mg/mL (293.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Junzhen Wu, et al. Evaluation of the Effect of Contezolid (MRX-I) on the Corrected QT Interval in a Randomized, Double-Blind, Placebo- and Positive-Controlled Crossover Study in Healthy Chinese Volunteers. Antimicrob Agents Chemother. 2020 May 21;64(6):e02158-19. [Content Brief]
[2]. Mikhail F Gordeev, et al. New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile. J Med Chem. 2014 Jun 12;57(11):4487-97. [Content Brief]
[3]. Carolyn Shoen, et al. In Vitro and In Vivo Activities of Contezolid (MRX-I) against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00493-18. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4490 mL | 12.2450 mL | 24.4900 mL | 61.2250 mL |
| 5 mM | 0.4898 mL | 2.4490 mL | 4.8980 mL | 12.2450 mL | |
| 10 mM | 0.2449 mL | 1.2245 mL | 2.4490 mL | 6.1225 mL | |
| 15 mM | 0.1633 mL | 0.8163 mL | 1.6327 mL | 4.0817 mL | |
| 20 mM | 0.1224 mL | 0.6122 mL | 1.2245 mL | 3.0612 mL | |
| 25 mM | 0.0980 mL | 0.4898 mL | 0.9796 mL | 2.4490 mL | |
| 30 mM | 0.0816 mL | 0.4082 mL | 0.8163 mL | 2.0408 mL | |
| 40 mM | 0.0612 mL | 0.3061 mL | 0.6122 mL | 1.5306 mL | |
| 50 mM | 0.0490 mL | 0.2449 mL | 0.4898 mL | 1.2245 mL | |
| 60 mM | 0.0408 mL | 0.2041 mL | 0.4082 mL | 1.0204 mL | |
| 80 mM | 0.0306 mL | 0.1531 mL | 0.3061 mL | 0.7653 mL | |
| 100 mM | 0.0245 mL | 0.1224 mL | 0.2449 mL | 0.6122 mL |
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