Shanghai Nianxing Industrial Co., Ltd
China
Product Name: ACHN-975 TFA
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Purity: 95.0%
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1410809-37-8

1410809-37-8 structure

1410809-37-8 structure

Name: ACHN-975 TFA
Chemical Name: ACHN-975 TFA
CAS Number: 1410809-37-8
Molecular Formula: C₂₂H₂₄F₃N₃O₆
Molecular Weight: 483.44
Catalog: Signaling Pathways Anti-infection Bacterial
Create Date: 2020-06-01 13:31:45
Modify Date: 2025-08-27 11:16:27
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].

Name	ACHN-975 TFA
Synonyms	MFCD29991589

Description	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].
Related Catalog	Research Areas >> Infection Signaling Pathways >> Anti-infection >> Bacterial
Target	IC50: LpxC[1]
In Vitro	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].
In Vivo	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] Dosage: 5-30 mg/kg Administration: Intraperitoneal administration; single dose Result: Had a bactericidal activity and was against the P. aeruginosa ATCC27853 strain in vivo.
References	[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.

Molecular Formula	C₂₂H₂₄F₃N₃O₆
Molecular Weight	483.44

Hazard Codes	Xi

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