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ACHN-975

Catalog No. T10236L   CAS 1410809-36-7

ACHN-975 is a highly potent and selective LpxC inhibitor, demonstrating subnanomolar inhibitory activity. It effectively targets a broad spectrum of gram-negative bacteria, with low minimum inhibitory concentration (MIC) values (≤1 μg/mL)[1].

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ACHN-975 Chemical Structure
ACHN-975, CAS 1410809-36-7
Pack Size Availability Price/USD Quantity
25 mg 10-14 weeks $ 2,870.00
50 mg 10-14 weeks $ 3,780.00
100 mg 10-14 weeks $ 5,200.00
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ACHN-975 is a highly potent and selective LpxC inhibitor, demonstrating subnanomolar inhibitory activity. It effectively targets a broad spectrum of gram-negative bacteria, with low minimum inhibitory concentration (MIC) values (≤1 μg/mL)[1].
In vitro ACHN-975 is against Enterobacteriaceae spp with an IC50 of 0.02 nM[1] and is against Enterobacteriaceae spp, Pa, and Ab with MIC90 values of 1, 0.5, and >64 μg/mL, respectively[1]. 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], it against Pseudomonas aeruginosa with an MIC50 and MIC90 of 0.06 and 0.25?μg/ml, respectively[2]. ACHN-975 is potently against the P. aeruginosa isolates tested, inhibiting 100% of the isolates at an MIC of ≤2?μg/ml. LpxC is highly conserved in gram-negative bacteria and catalyzes the first committed step of lipid A biosynthesis and is the bacterial enzyme Zinc-dependent metalloamidase UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase[1].
In vivo ACHN-975 (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, which 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].
Molecular Weight 369.41
Formula C20H23N3O4
CAS No. 1410809-36-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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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Keywords

ACHN-975 1410809-36-7 Others ACHN 975 ACHN975 inhibitor inhibit

 

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