Sutezolid
Based on 4 publication(s) in Google Scholar
Sutezolid (PNU-100480), an orally active oxazolidinone antimicrobial agent, acts by inhibiting bacterial protein synthesis. Sutezolid has potent activity against mycobacteria, and is used for the research of drug-resistant tuberculosis.
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- Pureza: 99.40%
- No. CAS: 168828-58-8
- Fòrmula: C16H20FN3O3S
- Peso molecular:353.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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Publications Citing Use of MedChemExpress (MCE) Sutezolid
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Actividad biológica
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Oxazolidinone |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| H9c2 | IC50 |
8.17 μM
Compound: Sutezolid
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Inhibition of mitochondrial protein synthesis in rat H9c2 cells measured after 5 days by ELISA
Inhibition of mitochondrial protein synthesis in rat H9c2 cells measured after 5 days by ELISA
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[PMID: 32666789] |
| HepG2 | IC50 |
>64 μg/mL
Compound: Sutezolid
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
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[PMID: 32666789] |
| MT4 | CC50 |
>100 μM
Compound: PNU-100480
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Cytotoxicity of compound against mock-infected MT-4 cells was evaluated by MTT assay
Cytotoxicity of compound against mock-infected MT-4 cells was evaluated by MTT assay
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[PMID: 15006398] |
| Vero | IC50 |
>64 μg/mL
Compound: Sutezolid
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
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[PMID: 32666789] |
Sutezolid (PNU-100480) exhibits excellent in vitro activity against multiple clinical isolates of Mycobacterium avium complex (MIC’s=0.5-4 μg/mL)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 168828-58-8
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Appearance Solid
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Peso molecular 353.41
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Fòrmula C16H20FN3O3S
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Color Pale purple to purple
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SMILES
O=C(O[C@H]1CNC(C)=O)N(C1)C2=CC(F)=C(N3CCSCC3)C=C2
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Synonyms
PNU-100480; U-100480; PF-02341272
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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
Publications (4)
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Journal Impact Factor
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Most Recent
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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 -
Antimicrob Agents Chemother
Heterologous Expression of ethA and katG in Mycobacterium marinum Enables the Rapid Identification of New Prodrugs Active against Mycobacterium tuberculosis. [Abstract]2021 Mar 18;65(4):e01445-20. PMID: 33495223 -
Dis Model Mech
An anti-tuberculosis compound screen using a zebrafish infection model identifies an aspartyl-tRNA synthetase inhibitor. [Abstract]2021 Dec 1;14(12):dmm049145. PMID: 34643222 -
J Pharm Biomed Anal
Characterization of degradation products and process-related impurity of sutezolid by liquid chromatography/electrospray ionization tandem mass spectrometry. [Abstract]2019 May 30:169:196-207. PMID: 30877931
Solvente y solubilidad
DMSO : 50 mg/mL (141.48 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 (7.07 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 (7.07 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 (275 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)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Barbachyn MR, et al. Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity. J Med Chem. 1996;39(3):680-685. [Content Brief]
[3]. Zhu T, et al. Population pharmacokinetic/pharmacodynamic analysis of the bactericidal activities of sutezolid (PNU-100480) and its major metabolite against intracellular Mycobacterium tuberculosis in ex vivo whole-blood cultures of patients with pulmonary tuberculosis. Antimicrob Agents Chemother. 2014;58(6):3306-3311. [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 | 2.8296 mL | 14.1479 mL | 28.2957 mL | 70.7394 mL |
| 5 mM | 0.5659 mL | 2.8296 mL | 5.6591 mL | 14.1479 mL | |
| 10 mM | 0.2830 mL | 1.4148 mL | 2.8296 mL | 7.0739 mL | |
| 15 mM | 0.1886 mL | 0.9432 mL | 1.8864 mL | 4.7160 mL | |
| 20 mM | 0.1415 mL | 0.7074 mL | 1.4148 mL | 3.5370 mL | |
| 25 mM | 0.1132 mL | 0.5659 mL | 1.1318 mL | 2.8296 mL | |
| 30 mM | 0.0943 mL | 0.4716 mL | 0.9432 mL | 2.3580 mL | |
| 40 mM | 0.0707 mL | 0.3537 mL | 0.7074 mL | 1.7685 mL | |
| 50 mM | 0.0566 mL | 0.2830 mL | 0.5659 mL | 1.4148 mL | |
| 60 mM | 0.0472 mL | 0.2358 mL | 0.4716 mL | 1.1790 mL | |
| 80 mM | 0.0354 mL | 0.1768 mL | 0.3537 mL | 0.8842 mL | |
| 100 mM | 0.0283 mL | 0.1415 mL | 0.2830 mL | 0.7074 mL |
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