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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Bacterial-JSF-3285
JSF-3285

Chemical Structure : JSF-3285

CAS No.:

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JSF-3285 (JSF3285)

货号: PC-20079Not For Human Use, Lab Use Only.

JSF-3285 (JSF3285) is a potent small molecule inhibitor of the M. tuberculosis β-ketoacyl synthase KasA with Kd of 70.7 nM in MST assays, shows activity against H37Rv strain with MIC 0.2 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    JSF-3285 (JSF3285) is a potent small molecule inhibitor of the M. tuberculosis β-ketoacyl synthase KasA with Kd of 70.7 nM in MST assays, shows activity against H37Rv strain with MIC 0.2 uM.
    JSF-3285 demonstrated whole-cell activity versus a panel of 48 drug-sensitive and drug-resistant clinical strains comparable with its efficacy versus the H37Rv strain (MIC, 0.2 uM).
    JSF-3285 dispplayed a 30-fold increase in mouse plasma exposure compared with GSK3011724A (DG167, Catalog# PC-35948).
    JSF-3285 (100 and 200 mg/kg qd po) achieved a ~2 log10 reduction in bacterial burden in  M. tuberculosis infection CD-1 mice.
    KasA is the only essential member of three β-ketoacyl synthases encoded in the M. tuberculosis genome.
    KasA catalyzes the 2-carbon elongation of growing fatty acyl chains in the FAS-II pathway, critical to the biosynthesis of mycolic acids and, in turn, the bacterial cell wall.

    物理化学性质&存储条件

    分子量 285.34
    分子式 C12H16FN3O2S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    4-fluoro-N-(3-methyl-1H-indazol-6-yl)butane-1-sulfonamide

    参考文献

    1. Inoyama D, et al. Cell Chem Biol. 2020 May 21;27(5):560-570.e10.

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