ACHN-975 TFA |
Catalog No.GC60039 |
L'ACHN-975 TFA est un inhibiteur sélectif de LpxC et présente une activité inhibitrice subnanomolaire de LpxC.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1410809-37-8
Sample solution is provided at 25 µL, 10mM.
ACHN-975 TFA is a selective LpxC inhibitor and exhibits a subnanomolar LpxC inhibitory activity. ACHN-975 TFA is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL)[1].
ACHN-975 is against Enterobacteriaceae spp with an IC50 of 0.02 nM[1].ACHN-975 is against Enterobacteriaceae spp, Pa, and Ab with MIC90 values of 1, 0.5, and >64 μg/mL, respectively[1].ACHN-975 is potently against the P. aeruginosa isolates tested, inhibiting 100% of the isolates at an MIC of ≤2 μg/ml. It against Pseudomonas aeruginosa with an MIC50 and MIC90 of 0.06 and 0.25 μg/ml, respectively[2].ACHN-975 is against six P. aeruginosa isolates, it against P. aeruginosa APAE1064, APAE1232, and APAE1064 isolates with MIC values of 0.12, 0.06 and 0.06 μg/ml, respectively[2].LpxC is highly conserved in gram-negative bacteria and catalyzes the first committed step of lipid A biosynthesis. LpxC is the bacterial enzyme Zinc-dependent metalloamidase UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase[1].
ACHN-975 TFA (intraperitoneal administration; 5-30 mg/kg; single dose) leads to a steady reduction in bacterial titers in the first 4 h following treatment for all dosing groups. The sampling shows that the level of free drug in this model drops below the ACHN-975 MIC for this isolate (0.25 μg/ml) by 2 h after treatment with the 10 mg/kg dose and by 4 h after treatment with the 30 mg/kg dose[2]. Animal Model: Neutropenic mouse thigh model with P. aeruginosa ATCC 27853[2]
[1]. Kalinin DV, et al. Insights into the Zinc-Dependent Deacetylase LpxC: Biochemical Properties and Inhibitor Design. Curr Top Med Chem. 2016;16(21):2379-430. [2]. Krause KM,et al. Potent LpxC Inhibitors with In Vitro Activity against Multidrug-Resistant Pseudomonas aeruginosa.Antimicrob Agents Chemother. 2019 Oct 22;63(11). pii: e00977-19.
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