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TP0586532

Chemical Structure : TP0586532

CAS No.: 2427584-96-9

TP0586532 (TP 0586532)

Catalog No.: PC-38175Not For Human Use, Lab Use Only.

TP0586532 (TP 0586532) is a novel non-hydroxamate inhibitor of UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC) with IC50 of 0.101 uM, shows MIC values 2 mg/mL and 4 mg/mL for E. coli ATCC 25922 and K. pneumoniae ATCC 13883.

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Biological Activity

TP0586532 (TP 0586532) is a novel non-hydroxamate inhibitor of UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC) with IC50 of 0.101 uM, shows MIC values 2 mg/mL and 4 mg/mL for E. coli ATCC 25922 and K. pneumoniae ATCC 13883.
TP0586532 is effective against carbapenem-resistant Klebsiella pneumoniae and does not pose a cardiovascular risk.
The MIC90 of TP0586532 against clinical isolates of carbapenem-resistant Klebsiella pneumoniae was 4 ug/mL.
TP0586532 also showed an in vivo efficacy against murine systemic, urinary tract and lung infection models caused by meropenem- or ciprofloxacin-resistant strains.
TP0586532 also reduces LPS release and IL-6 production both in vitro and in vivo.

Physicochemical Properties

M.Wt 460.534
Formula C26H28N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((1R,5S,6s)-6-((4-(3-((2-((S)-1-hydroxyethyl)-1H-imidazol-1-yl)methyl)isoxazol-5-yl)phenyl)ethynyl)-3-azabicyclo[3.1.0]hexan-3-yl)butanoic acid

References

1. Ushiyama F, et al. Bioorg Med Chem. 2021 Jan 15;30:115964.

2. Fujita K, et al. J Antibiot (Tokyo). 2022 Feb;75(2):98-107. 

3. Fujita K, et al. J Antibiot (Tokyo). 2022 Mar;75(3):136-145. 

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