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编 号:F623620
分子式:C22H24F3N3O6
分子量:483.44
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
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).

体内研究:
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.Animal Model:Neutropenic mouse thigh model with?P. aeruginosa?ATCC 27853
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.

体外研究:
ACHN-975 is against Enterobacteriaceae spp with an IC50 of 0.02 nM.ACHN-975 is against Enterobacteriaceae spp, Pa, and Ab with MIC90 values of 1, 0.5, and >64 μg/mL, respectively.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.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.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.
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