Chemical Structure : LEI-800
CAS No.:
3040218-10-5
LEI-800
(LEI 800)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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444.55
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Formula
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C25H24N4O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(((2S,5R)-5-(4-(pyridin-3-yl)phenyl)pyrrolidin-2-yl)methyl)isoquinoline-5-sulfonamide
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References
1. Alexander T Bakke, et al. Nat Chem. 2024 Jun 19. doi: 10.1038/s41557-024-01516-x.
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