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.
For research use only. We do not sell to patients.
- CAS No.: 2706576-88-5
- Formula: C16H19F2N3O6S
- Molecular Weight:419.40
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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. Further protocols information, click here.
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2706576-88-5
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Molecular Weight 419.40
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MK-7762 Related Classifications
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