2. Anti-infection
  3. Bacterial Beta-lactamase
  4. 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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MBL-IN-5 Chemical Structure

MBL-IN-5 Chemical Structure

CAS No. : 2876921-34-3

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MBL-IN-5 Related Antibodies

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Description

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[1].

IC50 & Target[1]

NDM-1

0.05 nM (IC50)

IMP-1

21 nM (IC50)

VIM-1

14 nM (IC50)

In Vitro

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.

MBL-IN-5 Related Antibodies
In Vivo

MBL-IN-5 (Compound 17u) (20-50 mg/kg, s.c., every 8 h for 3 times) significantly increases the activity of IPM against carbapenem-resistant NDM-1-expressing Klebsiella pneumonia ATCC BAA 2146 and reduces the bacterial load in the neutropenic murine thigh infection model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: alone: 50 mg/kg, combination: 10 mg/kg IPM + 20 mg/kg MBL-IN-5
Administration: s.c., following 2 h postinfection, every 8 h for 3 times and then collects thighs to compare the CFU at 26 h.
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.
Molecular Weight

353.80

Formula

C20H16ClNO3
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MBL-IN-5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MBL-IN-52876921-34-3BacterialBeta-lactamaseβ-lactamaseInhibitorsAntimicrobialNeutropenic murine thigh infection modelImipenem (IPM)Inhibitorinhibitorinhibit

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