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Purity: ≥98%
Contezolid (Youxitai; MRX-I) is an orally bioavailable oxazolidinone-based antibacterial agent potentially for the treatment of acute bacterial skin. It acts as a protein synthesis inhibitor. Contezolid (Youxitai) was developed by Shanghai MicuRx Pharmaceuticals to treat drug-resistant bacteria such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). As of 2021, it has been approved in China as an antibiotic.
| ln Vitro |
Contezolid (MRX-I) is extremely efficient against all clinical isolates of Gram-positive Staphylococcus, Streptococcus, and Enterococcus, including multidrug-resistant (MDR) pathogens including MRSA, PRSP, MRSA, and VRE[2].
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| ln Vivo |
In mice, rats, and dogs, Contezolid (MRX-I) is rapidly absorbed through the mouth; peak plasma concentrations are seen 0.5–2.6 hours after dosing. The following dose-normalized Cmax/dose values were found for mice, rats, and dogs: 524, 1065, and 259 ng/mL/(mg/kg); 1654, 3703, and 1664 ng·h/mL/(mg/kg); T1/2 values were found to be 1, 1.5, and 3 hours; and oral bioavailability was found to be 69%, 109%, and 37%, respectively [2]. There is no overt toxicity seen with contezolid (MRX-I) [2]. Comparing untreated early and late controls to contezolid (MRX-I, 100 mg/kg once daily), the lung bacterial burden was considerably lower [3].
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| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse are intranasally infected with Mycobacterium tuberculosis Erdman[3].
Doses: 100, 50 (twice), 25 (twice) mg/kg. Route of Administration: intragastric (po) (po)administration, once or twice (two times) daily, five days a week for four weeks. Experimental Results: CFU recovered from the lungs was Dramatically lower (P < 0.05) compared with early and late control mice. MRX-I at 50 mg/kg and 25 mg/kg twice (two times) daily was Dramatically better than late-stage control mice (P < 0.05). MRX-I at 100 mg/kg one time/day was Dramatically better than 50 mg/kg and 25 mg/kg twice (two times) daily (P < 0.05). There was no statistical difference between 50 mg/kg MRX-I and 25 mg/kg twice (two times) daily (P > 0.05). Animal/Disease Models: Rat[2]. Doses: 20, 100 and 200/300 mg/kg/day. Doses: Take orally twice (two times) daily. Experimental Results: No deaths were observed. |
| 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.
[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. [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. |
| Molecular Formula |
C18H15F3N4O4
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|---|---|
| Molecular Weight |
408.331314325333
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| CAS # |
1112968-42-9
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| Related CAS # |
Contezolid acefosamil sodium;1807365-35-0;Contezolid phosphoramidic acid;1807365-43-0;Contezolid acefosamil;1807497-11-5
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
FC1C(=C(C(=CC=1N1C(=O)O[C@@H](CNC2C=CON=2)C1)F)N1C=CC(CC1)=O)F
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~120 mg/mL (~293.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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