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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2851907-60-1
- 分子式: C30H37N9O5S2
- 分子量:667.80
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
54 μM
|
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.
|
38579010 |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2851907-60-1
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分子量 667.80
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)