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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- CAS. Nr.: 2876921-34-3
- Formel: C20H16ClNO3
- Molecular Weight:353.80
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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NDM-1 0.05 nM (IC50) |
IMP-1 21 nM (IC50) |
VIM-1 14 nM (IC50) |
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.
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.
Chemical Information
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CAS. Nr. 2876921-34-3
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Molecular Weight 353.80
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MBL-IN-5 Related Classifications
HY-173472 Related Classifications
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