YL6113
YL6113 is a potent and selective dual inhibitor of metallo-β-lactamases (MBLs) and serine-β-lactamases (SBLs). YL6113 shows inhibitory effect to MBLs, such as NDm-1, VIM-2, IMP-1, with IC50 values of 0.25, 27.16 and 3.55 μM. YL6113 shows inhibitory effect to SBLs, such as KPC-2, AmpC, OXA-48, with IC50 values of 0.2, 34.1 and 1.31 μM. YL6113 enhances the antibacterial efficacy of Meropenem (HY-13678) against carbapenem-resistant Gram-negative bacteria. YL6113 can be used for the research of infection.
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。
- 分子式: C18H18BClN4O5
- 分子量:416.62
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Beta-lactamase アイソフォーム固有の製品をすべて表示
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生物活性
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KPC-2 0.2 μM (IC50) |
NDM-1 0.25 μM (IC50) |
OXA-48 1.31 μM (IC50) |
IMP-1 3.55 μM (IC50) |
VIM-2 27.16 μM (IC50) |
AmpC 34.1 μM (IC50) |
| Species | Dose | Route | T1/2 | Cmax | Tmax | AUC0-t | MRT0-t | Vz | ClF_obs |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 0.88 h | 4779.52 μg/L | 0.08 h | 3670.17 μg/L·h | 1.01 h | 3.46 L/kg | 2.72 L/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine sepsis model infected with NDM-1-producing K.p. 140509 strain[1]
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Dosage:10 mg/kg
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Administration:Ip, a single dose
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Result:Significantly reduced bacterial load in the lungs, liver, and kidneys compared to the control and Meropenem-only groups.
化学情報
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分子量 416.62
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分子式 C18H18BClN4O5
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SMILES
NCC1=CC=C(C=C1)C2=CN(N=N2)CC3=CC=C4OCB(OC4=C3C(O)=O)O.Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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)