1. Anti-infection
  2. Bacterial
  3. Antitubercular agent-32

Antitubercular agent-32 是一种 Benzothiazinone (HY-13579A) 衍生物,能够抑制结核分枝杆菌 M. tuberculosis,并具有代谢稳定性和良好水溶性。Antitubercular agent-32 能够靶向 decaprenylphosphoryl-β-D-ribose 2’-氧化酶 (DprE1, IC50=3.9 μM) 来行使抗结核作用。

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Antitubercular agent-32 Chemical Structure

Antitubercular agent-32 Chemical Structure

CAS No. : 2498762-42-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antitubercular agent-32 is a derivate of Benzothiazinone (HY-13579A), inhibits M. tuberculosis, and shows improved metabolic stability and enhanced water solubility. Antitubercular agent-32 exerts antitubercular effect by targeting decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, IC50=3.9 μM)[1].

体外研究
(In Vitro)

Antitubercular agent-32 (compound 8) (0-7.5 mg/mL; 48 h) shows low cytotoxicity and inhibits M. tuberculosis H37Rv with the minimum inhibition concentration (MIC) of 40 nM[1].
Antitubercular agent-32 (0-20 μM) inhibits decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, 0.5 μM), an enzyme essential for the biosynthesis of mycobacterial cell wall, with an IC50 value of 3.9 μM[1].
Antitubercular agent-32 (1 μM; 10 min) exhibits metabolic stability in the liver microsomal metabolic of both human (HLM) and mouse (MLM), with fast clearance rates of 77 mL/min/kg (HLM) and 163 mL/min/kg (MLM), respectively[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 cells
Concentration: 0, 15, 30, 75, 150, 300, 750, 1500, 3000, and 7500 ng/mL
Incubation Time: 48 hours
Result: There were no significantly growth inhibitions of HepG2 cells.
分子量

492.61

Formula

C22H28N4O5S2

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

Antitubercular agent-32 相关分类

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  • 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.

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产品名称:
Antitubercular agent-32
目录号:
HY-151340
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