MBL-IN-5
MBL-IN-5 is a metallo-β-lactamase (MBL) inhibitor. MBL-IN-5 inhibits three clinically relevant B1 subfamily MBLs (NDM-1, VIM-1, and IMP-1) with IC50s of 0.05 nM, 14 nM and 21 nM respectively. MBL-IN-5 remarkably enhances carbapenems’ effectiveness against MBL-producing clinical strains and significantly reduces the bacterial load in a neutropenic murine thigh infection model combined with the IPM antibiotic.
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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: 2876921-34-3
- 分子式: C20H16ClNO3
- 分子量:353.80
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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
製品説明
IC50 & Target
[1]|
NDM-1 0.05 nM (IC50) |
IMP-1 21 nM (IC50) |
VIM-1 14 nM (IC50) |
体外実験
MBL-IN-5 (Compound 17u) (4-32 μg/mL, 16-18 h) exhibits strong synergy with Imipenem (IPM) (HY-B1369A) and Meropenem (HY-13678) against the New Delhi metallo-β-lactamase-1 (NDM-1)-expressing carbapenem-resistant Klebsiella pneumoniae ATCC BAA-2146[1].
MBL-IN-5 (3.12-50 μM) potently stabilizes NDM-1 with a positive shift in Tm of about ~15-20 °C[1].
MBL-IN-5 (1-500 μM) has desirable ADME properties, exhibiting moderate solubility, high permeability and medium clearance[1].
MBL-IN-5 (0.5-16 μg/mL, 16-18 h) effectively inhibits NDM-1, restoring susceptibility to IPM and Meropenem (MIC reduction by several-fold) in all tested ATCC strains and the combination with either IPM or Meropenem can highly inhibit NDM-1-producing Enterobacteriaceae clinical strains[1].
MBL-IN-5 has a high degree of specificity for MBLs over MMPs with IC50 of >120 μM, 2.9 μM, and 45 μM for MMP-1, MMP-2, and MMP-9, respectively[1].
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.
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Animal Model:female BALB/c mice (6-8 weeks old) were given two intraperitoneal cyclophosphamide injections 4 days and 1 day and then injected into the left thighs with 0.05 mL diluted culture of NDM-1 expressing Klebsiella pneumonia ATCC BAA 2146 (5 × 105 CFU/ mouse)[1].
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Dosage:alone: 50 mg/kg, combination: 10 mg/kg IPM + 20 mg/kg MBL-IN-5
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Administration:s.c., following 2 h postinfection, every 8 h for 3 times and then collects thighs to compare the CFU at 26 h.
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Result:Enhanced the activity of IPM against carbapenem-resistant NDM-1-expressing Klebsiella pneumonia ATCC BAA 2146 and significantly reduced ~2.2 log10 CFU/mL/thigh combined with IPM.
化学情報
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CAS 番号 2876921-34-3
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分子量 353.80
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分子式 C20H16ClNO3
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SMILES
O=C(C1=C(C2=C(OC)C=CC(Cl)=C2)C3=C(C4=C(CC3)C=CC=C4)N1)O
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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)
MBL-IN-5 関連分類
HY-173472 関連分類
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