企业信息

    苏州艾希文化学有限公司

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  • 公司认证: 营业执照已认证
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  • 公司地址: 江苏省 苏州 工业园区维新路
  • 姓名: 陆经理
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    供应分类

    Pa-824

  • 所属行业:化工 **化工原料 特殊/专业**化工原料
  • 发布日期:2016-12-10
  • 阅读量:291
  • 价格:1200.00 元/克 起
  • 产品规格:不限
  • 产品数量:1000.00 克
  • 包装说明:不限
  • 发货地址:江苏苏州  
  • 关键词:PA-824

    Pa-824详细内容

    PA-824(Pretomanid) 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]
    Target: tuberculosis
    PA-824 exhibited a sub-micromolar minimal inhibitory concentration (MIC) against MTB, Although 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 -1. This indicated that 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 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]. PA-824 showed significant activity at 2, 10, and 50 microg/ml, similar to that of metronidazole, in a dose-dependent manner. 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 PA-824 at 100 mg/kg in cyclodextrin/lecithin reduced the bacterial load below 500 CFU in the lungs and spleen [2]. 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].
    

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