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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C14H10Cl2N6O
- 分子量:349.17
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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.
化学情報
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分子量 349.17
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
- 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