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  3. ACHN-975 TFA

ACHN-975 TFA 

Cat. No.: HY-19936A Purity: >95.0%
Handling Instructions

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).

For research use only. We do not sell to patients.

ACHN-975 TFA Chemical Structure

ACHN-975 TFA Chemical Structure

CAS No. : 1410809-37-8

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5 mg USD 395 In-stock
Estimated Time of Arrival: December 31
10 mg USD 670 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

483.44

Formula

C₂₂H₂₄F₃N₃O₆

CAS No.

1410809-37-8

SMILES

O=C(N[[email protected]](C(NO)=O)C(C)(N)C)C1=CC=C(C#CC#C[[email protected]]2[[email protected]](CO)C2)C=C1.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References

Purity: >95.0%

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Keywords:

ACHN-975ACHN975ACHN 975BacterialP. aeruginosainfectionEnterobacteriaceaeAPAE1064APAE1232LpxCInhibitorinhibitorinhibit

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ACHN-975 TFA
Cat. No.:
HY-19936A
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