EBL-3647
EBL-3647 is a LpxH inhibitor derived from JEDI-1444 (HY-187940) that blocks the essential manganese-dependent UDP-diacylglucosamine pyrophosphatase in lipid A biosynthesis. EBL-3647 exhibits antibacterial activity against wild-type E. coli and K. pneumoniae, and shows measurable MICs against efflux-deficient A. baumannii, P. aeruginosa, and P. mirabilis. EBL-3647 demonstrates in vivo efficacy against E. coli and K. pneumoniae in a mouse peritonitis model. EBL-3647 can be used for research on bacterial infections and peritonitis.
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- CAS No.: 2851907-60-1
- Formule: C30H37N9O5S2
- Masse moléculaire:667.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
54 μM
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Cytotoxicity against human HepG2 hepatoma cells assessed as viability reduction incubated 72 hrs by fluorometric microculture cytotoxicity assay.
Cytotoxicity against human HepG2 hepatoma cells assessed as viability reduction incubated 72 hrs by fluorometric microculture cytotoxicity assay.
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38579010 |
In Vitro
EBL-3647 (4× MIC) selects for spontaneous resistance at a frequency of 5.4 × 10-10 in K. pneumoniae ATCC 13883 and at a frequency of < 8.5 × 10-10 in E. coli 25922[1].
EBL-3647 inhibits E. coli LpxH with an IC50 of 2.2 nM; the reported MIC against E. coli 25922 is 2.0 μg/mL[2].
EBL-3647 inhibits E. coli LpxH with an IC50 of 2.2 nM[3].
EBL-3647 inhibits the growth of E. coli ATCC 25922 with an MIC of 2 mg/L, and has an MIC of ≤0.125 mg/L against the ΔtolC efflux mutant; it inhibits K. pneumoniae ATCC 13883 with an MIC of 0.5 mg/L, and 0.25 mg/L in 50% human serum[3].
EBL-3647 has an MIC90 of 4 mg/L against E. coli isolates and 8 mg/L against K. pneumoniae isolates[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2851907-60-1
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Masse moléculaire 667.80
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Formule C30H37N9O5S2
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SMILES
N#CC1=CC(C)=NC(N2CCN(S(=O)(C3=CC=C(NC(C4=CC(CN5CC(C5)CN)=CC=C4N(S(=O)(C)=O)C)=O)C=C3)=O)CC2)=N1
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EBL-3647 Related Classifications
HY-187938 Related Classifications
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