Antimycobacterial agent-18
Antimycobacterial agent-18 is a mycobacterial Fatty Acid Synthase I (FAS I) system inhibitor. Antimycobacterial agent-18 shows antimycobacterial activity against Mycobacterium tuberculosis H37Ra and drug-resistant Mycobacterium tuberculosis isolates, and partial activity against Mycobacterium abscessus. Antimycobacterial agent-18 can be used for the research of tuberculosis.
For research use only. We do not sell to patients.
- Formula: C14H10Cl2N6O
- Molecular Weight:349.17
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Antimycobacterial agent-18 (Compound 7) potently inhibits growth of Mycobacterium smegmatis (MIC = 15.63 μg/mL), M. aurum (MIC = 31.25 μg/mL), M. avium (MIC = 15.63 μg/mL), M. kansasii (MIC = 7.81 μg/mL), Mtb H37Ra (MIC = 1.98 μg/mL), and Mtb H37Rv (MIC = 6.25 μg/mL)[1].
Antimycobacterial agent-18 (14-21 days) retains activity against multiple drug-resistant Mtb clinical isolates, with MIC values ranging from 3.13 μg/mL to 87.29 μg/mL, and inhibits naturally resistant M. abscessus with an MIC of 25 μg/mL[1].
Antimycobacterial agent-18 (28 days) does not exhibit reduced potency against Mtb H37Ra strains overproducing FAS II enzymes InhA or HadABC, confirming its mechanism of action is unrelated to the FAS II system[1].
Antimycobacterial agent-18 (24 h) has low cytotoxicity in HepG2 cells (IC50 = 106.1 μM) with favorable selectivity indices for Mtb H37Ra (SI = 18.71) and Mtb H37Rv (SI = 5.92), and higher cytotoxicity in HK-2 cells (IC50 = 59.1 μM)[1].
Antimycobacterial agent-18 (3.91-500 μM; 1 h) induces significant hemolysis of human erythrocytes only at 500 μM, exhibiting a far favorable erythrocyte safety profile[1].
Antimycobacterial agent-18 (1-100× MIC) inhibits fatty acid and derived lipid biosynthesis in Mtb H37Ra, without affecting mycolic acid, TDM, or TMM synthesis, consistent with interference with the FAS I system[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.
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Animal Model:larvae[1]
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Dosage:50-1500 mg/kg
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Administration:intrahemocoel; single dose
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Result:Induced 40% larval mortality within 24 hours post-administration at 1500 mg/kg.
Caused mortality over the 5-day observation period at 500 mg/kg.
Showed no larval mortality at 50 mg/kg.
Did not reach an LD at the maximum tested concentration.
Chemical Information
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Molecular Weight 349.17
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Formula C14H10Cl2N6O
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SMILES
O=C(C1=NC=C(Cl)N=C1)NCC2=CN(C3=CC=CC=C3Cl)N=N2
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Antimycobacterial agent-18
- Antimycobacterial agent18
- Antimycobacterial agent 18
- Bacterial
- Fatty Acid Synthase (FASN)
- HepG2 cells
- Mycobacterium tuberculosis H37Ra
- drug-resistant Mycobacterium tuberculosis isolates
- fatty acid biosynthesis
- mycolic acid synthesis
- Mycobacterium abscessus
- human erythrocytes
- human liver microsomes
- HK-2 cells
- Fatty Acid Synthase I (FAS I) system
- Inhibitor
- inhibitor
- inhibit