Contezolid acefosamil sodium
Based on 1 Customer Validation
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.
- Purity: 95.19%
- CAS No.: 1807365-35-0
- Formula: C20H17F3N4NaO8P
- Molecular Weight:552.33
-
Storage:
-80°C, stored under nitrogen
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
All Antibiotic Isoforms
More
Biological Activity
|
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.
-
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.
Chemical Information
-
CAS No. 1807365-35-0
-
Appearance Solid
-
Molecular Weight 552.33
-
Formula C20H17F3N4NaO8P
-
Color Off-white to light yellow
-
SMILES
FC(C(F)=C1N(C=C2)CCC2=O)=C(N(C(O3)=O)C[C@@H]3CN(C4=NOC=C4)[P](OC(C)=O)(O[Na])=O)C=C1F
-
Synonyms
MRX-4 sodium
-
Shipping
Shipping with dry ice.
-
Storage
-80°C, stored under nitrogen
Solvent & Solubility
DMSO : 180 mg/mL (325.89 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months.
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months.
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: ≥ 4.5 mg/mL (8.15 mM); Clear solution
This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 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: ≥ 4.5 mg/mL (8.15 mM); Clear solution
This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
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.
Purity & Documentation
-
Data Sheet (278 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
[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 (stored under nitrogen). When stored at -80°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8105 mL | 9.0526 mL | 18.1051 mL | 45.2628 mL |
| 5 mM | 0.3621 mL | 1.8105 mL | 3.6210 mL | 9.0526 mL | |
| 10 mM | 0.1811 mL | 0.9053 mL | 1.8105 mL | 4.5263 mL | |
| 15 mM | 0.1207 mL | 0.6035 mL | 1.2070 mL | 3.0175 mL | |
| 20 mM | 0.0905 mL | 0.4526 mL | 0.9053 mL | 2.2631 mL | |
| 25 mM | 0.0724 mL | 0.3621 mL | 0.7242 mL | 1.8105 mL | |
| 30 mM | 0.0604 mL | 0.3018 mL | 0.6035 mL | 1.5088 mL | |
| 40 mM | 0.0453 mL | 0.2263 mL | 0.4526 mL | 1.1316 mL | |
| 50 mM | 0.0362 mL | 0.1811 mL | 0.3621 mL | 0.9053 mL | |
| 60 mM | 0.0302 mL | 0.1509 mL | 0.3018 mL | 0.7544 mL | |
| 80 mM | 0.0226 mL | 0.1132 mL | 0.2263 mL | 0.5658 mL | |
| 100 mM | 0.0181 mL | 0.0905 mL | 0.1811 mL | 0.4526 mL |
Contezolid acefosamil sodium Related Classifications
HY-19915B Related Classifications
Powered by Bioz