Chemical Structure : Debio 1453
CAS No.:
2422053-29-8
Debio 1453
Catalog No.: PC-25529Not For Human Use, Lab Use Only.
Debio 1453 is a potent, selective inhibitor of Neisseria gonorrhoeae FabI (NgFabI) with IC50 of 0.6 nM, shows highly potent antibacterial activity against N. gonorrhoeae with MIC of 0.03 ug/mL.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Debio 1453 is a potent, selective inhibitor of Neisseria gonorrhoeae FabI (NgFabI) with IC50 of 0.6 nM, shows highly potent antibacterial activity against N. gonorrhoeae with MIC of 0.03 ug/mL.
Debio 1453 exhibits MIC range from 0.008 to 0.125 ug/mL against 100 consecutive, contemporary clinical N. gonorrhoeae isolates.
Debio 1453 displays rapid bactericidal killing against both antibiotic-susceptible and extensively drug-resistant (XDR) N. gonorrhoeae achieving ≥3 log10 reductions in viable CFU counts within 24 h in time-kill assays (>2 MIC).
Debio 1453 demonstrates low potential for toxicity in vitro.
Debio 1453 P (Debio 1453 phosphate prodrug) (80 mg/kg) demonstrates efficacy in N. gonorrhoeae-infected mice.
Physicochemical Properties
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M.Wt
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420.47
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Formula
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C23H24N4O4
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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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(E)-3-((2R,3S)-3-hydroxy-2-methyl-4-oxo-2,3,4,5-tetrahydro-1H-pyrido[2,3-b][1,4]diazepin-8-yl)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)acrylamide
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References
1. Gerusz V, et al. Nat Commun. 2025 Sep 18;16(1):8309.
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