2. Anti-infection
  3. Bacterial
  4. Antituberculosis agent-10

Antituberculosis agent-10 (Compound 9) 具有对 Mycobacterium tuberculosis 的抗菌活性 (MIC = 0.3 μM)。通过靶向细菌的 50S 核糖体亚基，抑制蛋白质合成，从而发挥其抗菌作用。Antituberculosis agent-10 还具有口服活性。

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Antituberculosis agent-10 Chemical Structure

Antituberculosis agent-10 Chemical Structure

CAS No. : 2095636-19-2

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Antituberculosis agent-10 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antituberculosis agent-10 (Compound 9) has excellent antibacterial activity against Mycobacterium tuberculosis (MIC = 0.3 μM). Antituberculosis agent-10 inhibits protein synthesis by targeting the 50S ribosomal subunit of the bacterium, thus exerting its antibacterial effect. Antituberculosis agent-10 is orally active[1].

体外研究
(In Vitro)

Antituberculosis agent-10 (72 h) 对 HepG2 细胞的线粒体蛋白合成 (MPS) 的抑制没有活性 (IC50 = 150 μM)，但其代谢产物显示出线粒体毒性[1]。

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

Antituberculosis agent-10 相关抗体:
体内研究
(In Vivo)

Antituberculosis agent-10 (i.g.; 5-50 mg/kg; 每天一次或者每天两次) 在感染 C3HeB/FeJ 小鼠内表现出优异的渗透性和持续的活性[1]。
Antituberculosis agent-10 ((i.g.; 4 mg/kg,每天两次持续一周,之后每天一次) 处理显著减少了 Mtb 感染的狨猴的结核病灶的体积，具有强大的抗菌活性[1]。


药代动力学分析[1]

Route Dose (mpk) Cl/Clu (mL/min/kg) Vd/Vdu (L/kg) MRT/ss t1/2 (h) F (%)
i.v. 2 12/316 0.6/16 0.8/0.6 /
p.o. 10 / / / 64

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

Animal Model: infected C3HeB/FeJ mice[1]
Dosage: 5,10,15,,50 mg/kg, twice daily; 30 mg/kg,once daily
Administration: i.g.
Result: Penetrated effectively into both the cellular and necrotic compartments of the lesions.
Maintained concentrations above the MIC for tuberculosis bacteria at various lesion sites.
Animal Model: Mtb-infected marmosets[1]
Dosage: 4 mg/kg, twice daily for 1 week then 4 mg/kg once daily
Administration: i.g.
Result: Reduced physical lesion size and bacterial load within those lesions.
Showed superior or at least comparable results in reducing lesion volume and bacterial count than linezolid (HY-10394).
分子量

364.39

Formula

C17H17FN2O4S
CAS 号
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

Antituberculosis agent-10 相关分类

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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:

Antituberculosis agent-102095636-19-2Antituberculosis agent10Antituberculosis agent 10Bacterialtuberculosisoxazolidinoneantibacterialpro-drugnonhuman primateInhibitorinhibitorinhibit

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