Eperezolid
Based on 1 Customer Validation
Eperezolid (PNU-100592) is an orally active protein synthesis inhibitor that targets the bacterial 50S ribosomal subunit. Eperezolid competitively binds to a specific site on the ribosomal 50S subunit (overlapping with the binding sites of chloramphenicol (HY-B0239) and lincomycin (HY-117660)) to inhibit the translation initiation stage and exert antibacterial activity. Eperezolid can induce host cell autophagy to enhance the clearance of intracellular mycobacteria, and its MIC90 for Staphylococcus aureus and Enterococcus is 1-4 μg/mL. Eperezolid is mainly used for antibacterial research on infections with Gram-positive bacteria such as methicillin-resistant (HY-121544) Staphylococci and vancomycin-resistant (HY-B0671) Enterococci, as well as infections with intracellular bacteria such as Mycobacterium tuberculosis.
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- Pureza: 96.55%
- No. CAS: 165800-04-4
- Fòrmula: C18H23FN4O5
- Peso molecular:394.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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Actividad biológica
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Oxazolidinone |
1. Antibacterial activity test: Eperezolid (1×MIC-4×MIC; 24 h) shows antibacterial activity in vitro against Methicillin-sensitive/resistant Staphylococcus aureus, coagulase-negative Staphylococci and Vancomycin-sensitive/resistant Enterococci with MIC90 of 1-4 μg/mL. Eperezolid exhibits an antibacterial effect and the post-antibiotic effect (PAE) against Enterococcus faecalis and Enterococcus faecium was 0.1-1.2 h[1].
2. Autophagy induction assay:
Eperezolid (1 μM; 24 h) induces autophagy in dTHP-1 cells, as evidenced by increased conversion of LC3-I to LC3-II, increased formation of LC3 puncta, and a significant increase in the number of autophagic vacuoles as confirmed by MDC staining. It also inhibits the survival of intracellular Mycobacterium smegmatis[1].
3. Ribosome binding assay:
Eperezolid (1-100 μM; 10 min) specifically binds to the 50S ribosomal subunit of Escherichia coli with a Kd of approximately 20 μM. Its binding can be competitively inhibited by chloramphenicol and lincomycin, but does not affect peptidyl transferase activity or translation termination[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Enterococcus faecium
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Concentration:1×MIC (1-4 μg/mL), 4×MIC
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Incubation Time:24 h
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Result:Showed bacteriostatic activity, with no significant reduction in bacterial counts (>1 log10 CFU/mL) over 24 h.
PAE was measured at 0.8 h against staphylococci and 0.1-0.8 h against enterococci, with higher PAE observed at 4×MIC.
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Cell Line:dTHP-1 human monocyte-derived macrophages
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Concentration:1 μM
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Incubation Time:24 h
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Result:Showed a significant increase in LC3-II/LC3-I ratio, and confocal microscopy revealed enhanced LC3 puncta formation.
MDC staining indicated a 2-fold increase in autophagic vacuoles compared to control.
Intracellular M. smegmatis viability was reduced by 50% compared to untreated controls.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (male, 175-250 g, 6-8 weeks old) with intra-abdominal abscess induced by Enterococcus faecalis 1310 or Vancomycin-resistant Enterococcus faecium A1221[3]
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Dosage:25 mg/kg
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Administration:Intravenous infusion or oral gavage, twice daily (q12h), for 4.5 days
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Result:For E. faecalis infection, had no significantly reduction in bacterial density in abscesses compared to untreated controls (mean viable bacteria: 8.3 log10 CFU/g vs. 8.6 log10 CFU/g).
For vancomycin-resistant E. faecium infection, i.v. eperezolid reduced bacterial density to 6.5 log10 CFU/g (vs. 8.25 log10 CFU/g in controls), while oral administration showed a modest reduction to 7.8 log10 CFU/g.
No sterile abscesses were observed in any treatment group.
Chemical Information
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No. CAS 165800-04-4
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Appearance Solid
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Peso molecular 394.40
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Fòrmula C18H23FN4O5
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Color White to off-white
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SMILES
O=C(O[C@H]1CNC(C)=O)N(C1)C2=CC(F)=C(C=C2)N3CCN(CC3)C(CO)=O
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Synonyms
PNU-100592
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 40 mg/mL (101.42 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (6.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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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.
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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Rybak MJ, et al. Comparative in vitro activities and postantibiotic effects of the oxazolidinone compounds eperezolid (PNU-100592) and linezolid (PNU-100766) versus vancomycin against Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus faecalis, and Enterococcus faecium. Antimicrob Agents Chemother. 1998 Mar;42(3):721-4. [Content Brief]
[3]. Schülin T, et al. Activities of the oxazolidinones linezolid and eperezolid in experimental intra-abdominal abscess due to Enterococcus faecalis or vancomycin-resistant Enterococcus faecium. Antimicrob Agents Chemother. 1999 Dec;43(12):2873-6. [Content Brief]
[4]. Lin AH, et al. The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin. Antimicrob Agents Chemother. 1997 Oct;41(10):2127-31. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5355 mL | 12.6775 mL | 25.3550 mL | 63.3874 mL |
| 5 mM | 0.5071 mL | 2.5355 mL | 5.0710 mL | 12.6775 mL | |
| 10 mM | 0.2535 mL | 1.2677 mL | 2.5355 mL | 6.3387 mL | |
| 15 mM | 0.1690 mL | 0.8452 mL | 1.6903 mL | 4.2258 mL | |
| 20 mM | 0.1268 mL | 0.6339 mL | 1.2677 mL | 3.1694 mL | |
| 25 mM | 0.1014 mL | 0.5071 mL | 1.0142 mL | 2.5355 mL | |
| 30 mM | 0.0845 mL | 0.4226 mL | 0.8452 mL | 2.1129 mL | |
| 40 mM | 0.0634 mL | 0.3169 mL | 0.6339 mL | 1.5847 mL | |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.5071 mL | 1.2677 mL | |
| 60 mM | 0.0423 mL | 0.2113 mL | 0.4226 mL | 1.0565 mL | |
| 80 mM | 0.0317 mL | 0.1585 mL | 0.3169 mL | 0.7923 mL | |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2535 mL | 0.6339 mL |
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