2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. ETX1975-3

ETX1975-3 是一种口服有效的结核分枝杆菌 (Mycobacterium tuberculosis) 细胞色素 bd 氧化酶抑制剂及杀菌剂。ETX1975-3 可破坏靶酶 b-血红素中心间的电子传递，与 Q203 (HY-101040) 联用对复制期及非复制期结核分枝杆菌均具杀菌活性，并能降低急性小鼠模型的细菌载量。ETX1975-3 对耐多药/广泛耐药结核分枝杆菌临床分离株及非结核分枝杆菌均保持活性，同时具备良好的临床前 ADMET 特征。ETX1975-3 可用于结核病与非结核分枝杆菌感染相关研究。

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ETX1975-3

ETX1975-3 Chemical Structure

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ETX1975-3 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].
体外研究
(In Vitro)

ETX1975-3 (3 μM) 具有良好的体外 ADMET 特性，在小鼠和人肝微粒体中代谢稳定性低，Caco-2 通透性低，且小鼠血浆蛋白结合率高[1]。
ETX1975-3 (1.7-5.0 μM; 15 h-5 d) 靶向脓肿分枝杆菌 Mycobacterium abscessus ΔqcrCAB 中的细胞色素 bd 氧化酶，其 ATP 耗竭的 IC50 为 1.7 μM，MIC50 为 5.0 μM[1]。
ETX1975-3 与 Q203 (100 nM) 具有协同抗菌效应，对牛分枝杆菌 BCG、结核分枝杆菌 H37Rv 以及鸟分枝杆菌中的细胞色素 bd 氧化酶，IC50 分别为 1.4 μM、0.5 μM、1.5 μM (ATP 耗竭实验)[1]。
ETX1975-3 (0.6-40 μM; 4 d) 与 250 nM Q203 联用时，可呈现剂量依赖性降低 THP-1 巨噬细胞内的结核分枝杆菌 N0145 载量[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ETX1975-3 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: ADME parameters in Caco-2 cells
Concentration: /
Incubation Time: /
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.
药代动力学
(Parmacokinetics)
Species Dose Route Bioavailability Tmax T1/2 Cmax AUClast CL Vss
Mice[1] 2 mg/kg i.v. / / 2.23 h 927.53 ng/mL 593.67 ng·h/mL 53.3 mL/min/kg 5.58 L/kg
Mice[1] 10 mg/kg p.o. 44 % 1.00 h 2.21 h 392 ng/mL 1312 ng·h/mL / /
体内研究
(In Vivo)

ETX1975-3 (50 mg/kg; 口服; 每天 1 次，每周 5 次; 2 周) 无法降低 BALB/cJ 小鼠体内 Mycobacterium tuberculosis N0145 的肺部载菌量；但与 Q203 联用时，可使小鼠肺部杆菌载量显著降低[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Tuberculosis infected model in BALB/cJ mice (female, 6-8 weeks old, intranasal infection with Mycobacterium tuberculosis N0145)[1]
Dosage: 50 mg/kg
Administration: p.o.; once daily for 5 consecutive days per week; 2 weeks
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.
分子量

366.82

Formula

C20H16ClFN4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ETX1975-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ETX1975-3Cytochrome P450CYPsMycobacterium bovis BCGcytochrome bd oxidaseMycobacterium aviumnontuberculous mycobacteriaMycobacterium abscessusTHP-1 macrophagesBALB/cJ miceMycobacterium tuberculosisMycobacterium tuberculosis N0145Mycobacterium tuberculosis H37RvInhibitorinhibitorinhibit

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