MK-7762
Based on 1 Customer Validation
MK-7762 is an orally active xazolidinone compound with antitubercular activity. MK-7762 inhibits MAO-B and mammalian mitochondrial protein synthesis. MK-7762 reduces lung bacterial burden in BALB/c mouse models of acute and chronic tuberculosis infection, penetrates caseous necrotic lung lesions in C3HeB/FeJ mice, and maintains concentrations above unbound MIC in lesion compartments. MK-7762 can be used for the research of tuberculosis.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.97%
- CAS No.: 2706576-88-5
- Formule: C16H19F2N3O6S
- Masse moléculaire:419.40
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
MK-7762 (0.93 μM; 7 days) inhibits 95% of Mycobacterium tuberculosis (Mtb) growth[1].
MK-7762 (72 h) inhibits mammalian mitochondrial protein synthesis in HepG2 cells with an IC50 of 98 μM[1].
MK-7762 (18.1 μM; 7 days) kills 99% of H37Rv cells [1].
MK-7762 (10 μM) inhibits MAO-B with an IC50 of 6.9 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MK-7762 (30-200 mg/kg; i.g.; once daily; 1 month) reduces lung bacterial burden in chronically infected BALB/c mice[1].
MK-7762 (100 mg/kg; i.g.; once daily, 5 days/week; 2.5 weeks) penetrates caseous necrotic lesions in C3HeB/FeJ mice at levels above the unbound MIC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old, specific-pathogen-free, acute Mtb infection)[1]
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Dosage:30 mg/kg; 100 mg/kg
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Administration:I.g.; once daily, twice daily; 12 days
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Result:Achieved 1.4-log reduction in lung CFUs (30 mg/kg once daily).
Achieved 4.5-log reduction in lung CFUs (100 mg/kg once daily).
Achieved 5.3-log reduction in lung CFUs (100 mg/kg twice daily) versus untreated controls.
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Animal Model:BALB/c (female, 6-8 weeks old, specific-pathogen-free, chronic Mtb infection)[1]
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Dosage:30 mg/kg; 100 mg/kg; 200 mg/kg
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Administration:I.g.; once daily; 1 month
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Result:Achieved 0.7-log reduction in lung CFUs (30 mg/kg).
Achieved 1.9-log reduction in lung CFUs (100 mg/kg).
Achieved 2.2-log reduction in lung CFUs (200 mg/kg) versus untreated controls.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2706576-88-5
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Appearance Solid
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Masse moléculaire 419.40
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Formule C16H19F2N3O6S
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Color White to off-white
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SMILES
COC(NC[C@H]1CN(C(O1)=O)C2=CC(F)=C(C(F)=C2)N3CCS(=O)(CC3)=O)=O
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Synonyms
TBD09
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (238.44 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 (protect from 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 (protect from 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)
Pureté et documentation
Références
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 (protect from 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3844 mL | 11.9218 mL | 23.8436 mL | 59.6090 mL |
| 5 mM | 0.4769 mL | 2.3844 mL | 4.7687 mL | 11.9218 mL | |
| 10 mM | 0.2384 mL | 1.1922 mL | 2.3844 mL | 5.9609 mL | |
| 15 mM | 0.1590 mL | 0.7948 mL | 1.5896 mL | 3.9739 mL | |
| 20 mM | 0.1192 mL | 0.5961 mL | 1.1922 mL | 2.9804 mL | |
| 25 mM | 0.0954 mL | 0.4769 mL | 0.9537 mL | 2.3844 mL | |
| 30 mM | 0.0795 mL | 0.3974 mL | 0.7948 mL | 1.9870 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5961 mL | 1.4902 mL | |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4769 mL | 1.1922 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3974 mL | 0.9935 mL | |
| 80 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7451 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5961 mL |
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