ACHN-975
Based on 1 publication(s) in Google Scholar
ACHN-975 is a selective LpxC inhibitor and exhibits a subnanomolar LpxC inhibitory activity. ACHN-975 is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL).
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- CAS No.: 1410809-36-7
- Formule: C20H23N3O4
- Masse moléculaire:369.41
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Stockage:
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Activité biologique
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Chemical Information
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Activité biologique
LpxC[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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Neutropenic mouse thigh model with P. aeruginosa ATCC 27853[2]
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Dosage:5-30 mg/kg
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Administration:Intraperitoneal administration; single dose
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Result:Had a bactericidal activity and was against the P. aeruginosa ATCC 27853 strain in vivo.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1410809-36-7
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Masse moléculaire 369.41
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Formule C20H23N3O4
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SMILES
O=C(N[C@H](C(NO)=O)C(C)(N)C)C1=CC=C(C#CC#C[C@H]2[C@H](CO)C2)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Infect Dis
Genetic and Chemical Screening Reveals Targets and Compounds to Potentiate Gram-Positive Antibiotics against Gram-Negative Bacteria. [Abstract]2022 Oct 14;8(10):2187-2197. PMID: 36098580
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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