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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Bacterial-LEI-800
LEI-800

Chemical Structure : LEI-800

CAS No.: 3040218-10-5

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LEI-800 (LEI 800)

货号: PC-22556Not For Human Use, Lab Use Only.

LEI-800 is potent antibacterial as an allosteric bacterial topoisomerase DNA gyrase inhibitor with MIC of 3.1 uM and 6.25 uM for E. coli and K. pneumoniae respectively, inhibits the ATP-dependent supercoiling activity of recombinant E. coli DNA gyrase in a gel-based assay with IC50 of 35 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LEI-800 is potent antibacterial as an allosteric bacterial topoisomerase DNA gyrase inhibitor with MIC of 3.1 uM and 6.25 uM for E. coli and K. pneumoniae respectively, inhibits the ATP-dependent supercoiling activity of recombinant E. coli DNA gyrase in a gel-based assay with IC50 of 35 nM.
LEI-800 shows selectivity towards the Gram-negative strains E. coli and K. pneumoniae when tested against a panel of pathogenic bacteria, maintains activity aginst several clinical isolates of E. coli.
LEI-800 directly interacts with DNA gyrase and blocks gyrase-dependent DNA cleavage。
LEI-800 binds a hydrophobic pocket within the GyrA subunit.
LEI-800 is active against fluoroquinolone-resistant clinical isolates.

物理化学性质&存储条件

分子量 444.55
分子式 C25H24N4O2S
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

N-(((2S,5R)-5-(4-(pyridin-3-yl)phenyl)pyrrolidin-2-yl)methyl)isoquinoline-5-sulfonamide

参考文献

1. Alexander T Bakke, et al. Nat Chem. 2024 Jun 19. doi: 10.1038/s41557-024-01516-x.

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