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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Bacterial-DS01750413
DS01750413

Chemical Structure : DS01750413

CAS No.: 2881067-92-9

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DS01750413 (DS 01750413)

货号: PC-47011Not For Human Use, Lab Use Only.

DS01750413 is a novel FtsZ inhibitor and new derivative of PC190723 (Cat. PC-47012), inhibits S. aureus FtsZ protein with IC50 of 2 mg/L, has an IC50 of 0.03 mg/L in cell elongation assay of B. subtilis.

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

    生物&药学活性

    DS01750413 is a novel FtsZ inhibitor and new derivative of PC190723 (Cat. PC-47012), inhibits S. aureus FtsZ protein with IC50 of 2 mg/L, has an IC50 of 0.03 mg/L in cell elongation assay of B. subtilis.
    DS01750413 shows no acitvity against mammalian tubulin (IC50>200 mg/L) and no any cytotoxicity concern.
    DS01750413 exhibitsa strong inhibitory activity against clinical isolates of S. aureus including MRSA and MSSA with an MIC range of 0.25-2 and 0.125-2 mg/L, respectively.
    DS01750413 also displays a similar activity against other Gram-positive bacteria, including MRSA strains that are resistant to current SOC antibiotics.
    DS01750413 displays a strong synergy specifically in combination with β-lactam antibiotics, but exhibits indifference effect with vancomycin and linezolid.
    DS01750413 shows no activity against G196S or N263S mutants (MIC>32 mg/L).
    DS01750413 (100 and 200 mg/kg, i.p.) showed a dose-dependent efficacy in the neutropenic murine bacteraemia infection model of S. aureus Smith.

    物理化学性质&存储条件

    分子量 488.217
    分子式 C18H13BrF3N3O5
    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

    (R)-5-(1-(5-bromo-4-(4-(trifluoromethoxy)phenyl)oxazol-2-yl)-2-hydroxyethoxy)nicotinamide

    参考文献

    1. Manoj Kumar, et al. J Antimicrob Chemother. 2021 Oct 11;76(11):2867-2874. 

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