ETX1975-3
ETX1975-3 is an orally active inhibitor and bactericide targeting the bd cytochrome oxidase of Mycobacterium tuberculosis. ETX1975-3 disrupts electron transfer between the b-heme centers of the target enzyme, and in combination with Q203 (HY-101040), exerts bactericidal activity against both replicating and non-replicating Mycobacterium tuberculosis, and reduces bacterial loads in acute mouse models. ETX1975-3 retains activity against clinical isolates of multidrug-resistant/extensively drug-resistant Mycobacterium tuberculosis and non-tuberculous mycobacteria, while possessing favorable preclinical ADMET properties. ETX1975-3 can be used in studies related to tuberculosis and non-tuberculous mycobacterial infections.
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: C20H16ClFN4
- 分子量:366.82
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保管条件:
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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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
ETX1975-3 (3 μM) exhibits favorable in vitro ADMET properties, with low metabolic stability in mouse and human liver microsomes, low Caco-2 permeability, and high plasma protein binding rate in mice[1].
ETX1975-3 (1.7-5.0 μM; 15 h-5 days) targets the cytochrome bd oxidase in Mycobacterium abscessus ΔqcrCAB, with an IC50 of 1.7 μM for ATP depletion and an MIC50 of 5.0 μM[1].
ETX1975-3 exerts a synergistic antibacterial effect with Q203 (100 nM), with IC50 values of 1.4 μM, 0.5 μM, and 1.5 μM against cytochrome bd oxidase in Mycobacterium bovis BCG, Mycobacterium tuberculosis H37Rv, and Mycobacterium avium, respectively (ATP depletion assay)[1].
Combination treatment with ETX1975-3 (0.6-40 μM; 4 d) and 250 nM Q203 dose-dependently reduces the load of Mycobacterium tuberculosis N0145 in THP-1 macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ADME parameters in Caco-2 cells
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Concentration:/
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Incubation Time:/
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Result:Exhibited low metabolic clearance (MLM and HLM ≤2.0 μl/min/mg), extremely low intestinal permeability (Caco2 Papp ≤3×10-6 cm/s), and high plasma protein binding (>99.9%) in in vitro ADME assays.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tuberculosis infected model in BALB/cJ mice (female, 6-8 weeks old, intranasal infection with Mycobacterium tuberculosis N0145)[1]
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Dosage:50 mg/kg
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Administration:p.o.; once daily for 5 consecutive days per week; 2 weeks
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Result:Became moribund by day 9 post-treatment and required sacrifice at day 10.
Produced a statistically significant reduction in lung bacillary loads when combined with Q203 compared to Q203 alone.
化学情報
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分子量 366.82
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分子式 C20H16ClFN4
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SMILES
CC1=NN2C3=CC(F)=CC=C3C(N[C@@H]4[C@H](C4)C5=CC=C(C=C5)Cl)=NC2=C1
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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)
ETX1975-3 関連分類
HY-181286 関連分類
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