MK-7762
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.
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- CAS. Nr.: 2706576-88-5
- Formel: C16H19F2N3O6S
- Molecular Weight:419.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2706576-88-5
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Molecular Weight 419.40
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Formel C16H19F2N3O6S
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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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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