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Art. -Nr.: HY-187895

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ME1071

ME1071 is a metallo-β-lactamase inhibitor. ME1071 inhibits IMP-1, VIM-2, and NDM-1 by blocking the entry of β-lactam compounds through zinc binding. ME1071 exhibits competitive inhibition against IMP-1 and VIM-2, and its activity against IMP-type enzymes is superior to that against NDM/VIM-type enzymes. ME1071 can be used in research on multidrug-resistant Gram-negative bacterial infections.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 13406-97-8
Formel: C₈H₁₂O₄
Molecular Weight:172.18

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

ME1071 Chemical Structure

CAS. Nr.: 13406-97-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]^[2]^[3]^[4]^[5]^{[6]

IMP-1
0.41 μM (Ki)

VIM-2
120 μM (Ki)

NDM-1

Alle Beta-lactamase Isoform-spezifische Produkte anzeigen :

Metallo-β-lactamase (MBL)

Serine β-lactamase (SBL)}

In Vitro

Bacterial InfectionOthers

Bacterial Infection

ME1071 reduces the carbapenem MICs of NDM-1-producing Enterobacteriaceae and Acinetobacter strains, but its synergistic effect is weaker than that in IMP- and VIM-producing bacteria^[1].
ME1071 (32 μg/mL; 16-18 h) increases the susceptibility of MBL-producing Pseudomonas aeruginosa (including IMP-1- and VIM-2-producing strains) to Ceftazidime (HY-B0593) and carbapenems and reduces their resistance, but has no significant effect on Piperacillin (HY-B1923) or Aztreonam (HY-B0129)^[2].
ME1071 (32 mg/L; 18 h) enhances the effect of Biapenem (HY-13573) against IMP-type MBL-producing Pseudomonas aeruginosa isolates^[5].

Others

ME1071 exhibits lower binding affinity for NDM-1 than for IMP-1 and VIM-2^[1].
ME1071 inhibits purified IMP-1 with a K_i of 0.41 μM and VIM-2 with a K_i of 120 μM in the nitrocefin hydrolysis assay^[2].

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

In Vivo

Bacterial InfectionCytokines & ChemokinesInnate Immunity

Bacterial Infection

Cytokines & Chemokines

Innate Immunity

ME1071 (100 mg/kg; intraperitoneal injection; twice daily; 7 days), in combination with Biapenem, reduces pulmonary bacterial burden and inflammation and prolongs survival in a mouse VAP model caused by MBL-producing Pseudomonas aeruginosa^[5].

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

Animal Model:

ddY (male, specific pathogen-free, 6 weeks old, 30-35 g)^[5]
Dosage:

100 mg/kg
Administration:

i.p.; every 12 h; 7 days; beginning 12 h after inoculation
Result:

Combination with Biapenem prolonged survival over 7 days compared with control and Biapenem alone.
Survival was not affected by single-agent administration.
At 30 h post infection, the combination with Biapenem group had 4.40 log₁₀ CFU/mL viable bacteria in lung homogenate (n = 6-7).
Histopathological examination showed only mild inflammatory changes in the combination with Biapenem group.
BALF total cell and neutrophil counts and IL-1β, IL-6, and TNFα levels were decreased in the combination with Biapenem group compared with control and Biapenem groups.

Related Protocols :

Gram Staining of Tissue Sections

Chemical Information

CAS. Nr. 13406-97-8
Molecular Weight 172.18
Formel C₈H₁₂O₄
SMILES

C(=C(\C(O)=O)/CC)(\C(O)=O)/CC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Xu ZQ, et al. Combating multidrug-resistant Gram-negative bacterial infections. Expert opinion on investigational drugs. 2014 Feb 1;23(2):163-82.

[2]. Ishii Y, et al. In vitro potentiation of carbapenems with ME1071, a novel metallo-beta-lactamase inhibitor, against metallo-beta-lactamase- producing Pseudomonas aeruginosa clinical isolates. Antimicrobial agents and chemotherapy. 2010 Sep;54(9):3625-9.

[3]. Bassetti M, et al. New treatment options against gram-negative organisms. Critical Care. 2011 Mar 22;15(2):215.

[4]. Wachino JI, et al. Sulfamoyl Heteroarylcarboxylic Acids as Promising Metallo-β-Lactamase Inhibitors for Controlling Bacterial Carbapenem Resistance. mBio. 2020 Mar 17;11(2):e03144-19.

[5]. Yamada K, et al. In vivo efficacy of biapenem with ME1071, a novel metallo-β-lactamase (MBL) inhibitor, in a murine model mimicking ventilator-associated pneumonia caused by MBL-producing Pseudomonas aeruginosa. International journal of antimicrobial agents. 2013 Sep;42(3):238-43.

[6]. Livermore DM, et al. Activity of carbapenems with ME1071 (disodium 2,3-diethylmaleate) against Enterobacteriaceae and Acinetobacter spp. with carbapenemases, including NDM enzymes. The Journal of antimicrobial chemotherapy. 2013 Jan;68(1):153-8.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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