NDM-1-IN-11
NDM-1-IN-11 is a potent covalent NDM-1 inhibitor with an IC50 of 1.12 μM, which acts by forming a Se-S bond with the enzyme. NDM-1-IN-11 effectively suppresses the growth of NDM-1-producing E. coli in both in vivo and in vitro models when combined with Meropenem (HY-13678). NDM-1-IN-11 can be used for addressing NDM-1 driven bacterial resistance.
For research use only. We do not sell to patients.
- Formula: C26H17FN2O4Se
- Molecular Weight:519.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Beta-lactamase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
NDM-1 1.12 μM (IC50) |
In Vitro
NDM-1-IN-11 (compound 27k) (24 h) demonstrates potent synergistic activity with Meropenem and exhibits an MIC of ≤32 µg/mL against NDM-1-producing Carbapenem-resistant Enterobacteriaceae (CRE) isolates[1].
NDM-1-IN-11 (0-64 μg/mL; 0-8 h) restores the efficacy of Meropenem against NDM-1-producing, Carbapenem resistant E. coli (strains ZJ487 and TG-1)[1].
NDM-1-IN-11 (0-64 μg/mL; 6 h) exhibits no significant cytotoxicity in HEK-293T and RAW264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HEK-293T, RAW264.7
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Concentration:0, 4, 8, 16, 32, 64 μg/mL
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Incubation Time:6 h
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Result:Showed no significant cytotoxicity in HEK-293T and RAW264.7 cells.
In Vivo
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 (6-8 weeks old, 18-22 g) intraperitoneally injected with E. coli ZJ487[1]
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Dosage:10 mg/kg
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Administration:s.c., every 12 hours, 3 doses
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Result:Did not significantly reduce bacterial counts in the liver and spleen of infected mice compared to the control group alone.
Resulted in a marked reduction in bacterial counts in the liver and spleen of infected mice when combined with Meropenem (10 mg/kg).
Chemical Information
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Molecular Weight 519.38
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Formula C26H17FN2O4Se
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SMILES
O=C1N([Se]C2=CC=C(C=C21)OCC3=CC=CC([N+]([O-])=O)=C3)C4=C(C=CC=C4)C5=CC=C(C=C5)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)