Pretomanid (PA-824) 可作用于肺结核

  • 来源:MedChemExpress LLC
  • 时间: 2019/12/31
  • 浏览人数: 320

    产品介绍:

     Pretomanid (PA-824) 可作用于肺结核,MIC为<1 μg/mL。 

    MCE 的所有产品仅用作科学研究,我们不为任何个人用途提供产品和服务

     目录号: HY-10844

     纯度: 99.53%

    作用机制:

    Pretomanid (PA-824) is a small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis; the MIC values of PA-824 against a panel of MTB pan-sensitive and rifampin mono-resistant clinical isolates ranged from 0.015 to 0.25 ug/ml. IC50 value: 0.015 to 0.25 ug/ml (MICs) [1]

    靶点:       Tuberculosis.

    体内实验参考:

     

    Pretomanid (PA-824) exhibited a sub-micromolar minimal inhibitory concentration (MIC) against MTB, Although Pretomanid (PA-824) was not the most potent NAP against cultured MTB clinical isolates, it was the most active in infected mice when orally administered at 25 mg/kg. This indicated that Pretomanid (PA-824) might possess more desirable pharmacokinetic properties than the other more potent NAP compounds that we tested. Further studies in mice at 25, 50 and 100 mg kg-1 Pretomanid (PA-824) daily for 10 days resulted in reductions of mycobacterial burden in both spleen and lung tissues that were comparable to that of INH at 25 mg kg -1 [1]. Pretomanid (PA-824) showed significant activity at 2, 10, and 50 microg/ml, similar to that of metronidazole, in a dose-dependent manner. Pretomanid (PA-824) at 100 mg/kg in cyclodextrin/lecithin was as active as moxifloxacin at 100 mg/kg and isoniazid at 25 mg/kg and was slightly more active than rifampin at 20 mg/kg. Long-term treatment with Pretomanid (PA-824) at 100 mg/kg in cyclodextrin/lecithin reduced the bacterial load below 500 CFU in the lungs and spleen [2]. Pretomanid (PA-824) has no effect on the viability of M. leprae in all three models, consistent with the lack of the nitroimidazo-oxazine-specific nitroreductase, encoded by Rv3547 in the M. leprae genome, which is essential for activation of this molecule [3].

    溶解方案:



    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

        1.

        请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

        Solubility: ≥ 2 mg/mL (5.57 mM); Clear solution

        2.

        请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

        Solubility: ≥ 2 mg/mL (5.57 mM); Clear solution

        3.

        请依序添加每种溶剂: 10% DMSO    90% corn oil

        Solubility: ≥ 2 mg/mL (5.57 mM); Clear solution

    *以上所有助溶剂都可在 MCE 网站选购。

    参考文献

    [1]. Stover CK, et al. A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature. 2000 Jun 22;405(6789):962-6.

    [2]. Lenaerts AJ, et al. Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. Antimicrob Agents Chemother. 2005 Jun;49(6):2294-301.

    [3]. Manjunatha UH, et al. Mycobacterium leprae is naturally resistant to PA-824. Antimicrob Agents Chemother. 2006 Oct;50(10):3350-4.

    PA-824 Pretomanid

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