MBL-IN-7
MBL-IN-7 is a potent metallo-β-lactamase (MBLs) inhibitor. The IC50 values of MBL-IN-7 against NDM-1, IMP-1, VIM-1, VIM-2, and L1 are 11 nM, 69 nM, 29 nM, 12 nM, and 85 μM, respectively. MBL-IN-7 is an antibiotic adjuvant. MBL-IN-7 competitively inhibits enzyme activity primarily by coordinating with zinc ions in the active site of MBLs and forming hydrogen bonds and π interactions, thereby protecting carbapenem antibiotics from hydrolysis. MBL-IN-7 is applicable to research related to carbapenem-resistant Gram-negative bacterial infections.
For research use only. We do not sell to patients.
- CAS No.: 3066273-36-4
- Formula: C19H14ClNO4
- Molecular Weight:355.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
NDM-1 11 nM (IC50) |
IMP-1 69 nM (IC50) |
VIM-1 29 nM (IC50) |
VIM-2 12 nM (IC50) |
L1 85 μM (IC50) |
In Vitro
MBL-IN-7 (compound 74) (up to 128 μg/mL) synergizes with Imipenem (HY-B1369A) and Meropenem (HY-13678) to restore their antibacterial activity in NDM-1-producing E. coli BAA-2471, K. pneumoniae BAA-2473, and A. baumannii BAA-3302[1].
The combination of MBL-IN-7 and Imipenem induces bacterial cell membrane rupture and cellular deformation in K. pneumoniae ATCC BAA-2473[1].
MBL-IN-7 potently inhibits the activity of purified NDM-1, IMP-1, VIM-1, VIM-2, and L1 metallo-β-lactamases, with IC50 values of 11 nM, 69 nM, 29 nM, 12 nM, and 85 μM, respectively[1].
MBL-IN-7 interacts with amino acid side chains and zinc ions in the active sites of the purified metallo-β-lactamase proteins NDM-1, IMP-1, and VIM-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | T1/2 | CLplasma | C0 | AUC0-last | AUC0-inf | MRT | Vss |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 5.0 mg/kg | i.v. | 4.11 h | 3.63 mL/min/kg | 24356.00 ng/mL | 19596.71 ng·h/mL | 19919.53 ng·h/mL | 4.93 h | 1.08 L/kg |
Chemical Information
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CAS No. 3066273-36-4
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Molecular Weight 355.77
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Formula C19H14ClNO4
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SMILES
O=C(O)C(N1)=C(C2=C(OC)C=CC(Cl)=C2)C3=C1C4=C(OC3)C=CC=C4
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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.
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)