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Art. -Nr.: HY-165460

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AM-112

AM-112 is a β-lactamase (β-lactamase) inhibitor and antibacterial agent, with IC₅₀ values ranging from 0.0002 μg/mL to 0.67 μg/mL against class A, C, and D β-lactamase. By inhibiting PBP2, the penicillin-binding protein of E. coli, and protecting Ceftazidime (HY-B0593) from enzymatic hydrolysis, AM-112 significantly enhances the antibacterial efficacy of Ceftazidime against Gram-negative bacteria, enterococci, and staphylococci. AM-112 exhibits favorable pharmacokinetic properties and acid-base stability. AM-112 can be used for the research of bacterial infections.

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CAS. Nr.: 414858-51-8
Formel: C₁₄H₂₂N₂O₅
Molecular Weight:298.34

Speicherung:

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

AM-112 Chemical Structure

CAS. Nr.: 414858-51-8

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

β-lactam

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In Vitro

AM-112 (combined with Ceftazidime at a 2:1 ratio) synergistically reduces the MIC of Ceftazidime (HY-B0593) in all tested Enterococcus faecalis strains, with the greatest MIC reduction observed in E. faecalis SFZ (from 64 μg/mL to 8 μg/mL)^[1].
AM-112 (0.5-32 μg/ml; 18-24 h) has an MIC of 2 μg/mL against Methicillin (HY-121544)-susceptible Staphylococcus aureus, an MIC range of 4-16 μg/mL against anaerobic bacteria of the genera Clostridium and Bacteroides, and an MIC of ≥32 μg/mL against Escherichia coli, Pseudomonas, Acinetobacter, Enterococcus and Methicillin-resistant Staphylococcus aureus^[2].

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

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay^[1]

Cell Line:

Multiple bacterial strains including Escherichia coli, Enterobacter cloacae, Enterococcus faecalis, Pseudomonas aeruginosa ATCC 27853 producing Class A or Class C β-lactamases
Concentration:

10 μg of AM-112 per disk, combined with 30 μg Ceftazidime per disk
Incubation Time:

overnight incubation at 37℃
Result:

Enhanced the zone diameter of Ceftazidime against bacterial isolates producing Class A and Class C β-lactamases, while it showed no enhancing effect on the activity of Ceftazidime against Pseudomonas aeruginosa ATCC 27853.

Parmacokinetics

Species	Dose	Route	Serum Concentration
Mice^[1]	50 mg/kg	s.c.	26 mg/L
Mice^[1]	50 mg/kg	p.o.	0 mg/L

In Vivo

AM-112 (administered subcutaneously at 1-2.6 mg/kg) exhibits potent inhibitory activity against Staphylococcus aureus-induced sepsis in mice, with an ED₅₀ of 2.6 mg/kg, and enhances the efficacy of Ceftazidime (HY-B0593) when used in combination^[1].
AM-112 (administered intravenously at 1.9-19 mg/kg) exhibits inhibitory effects against E. cloacae P99-induced sepsis in mice, with an ED₅₀ of 19 mg/kg, and significantly enhances the efficacy of Ceftazidime when co-administered^[1].
AM-112 (>40 mg/kg; s.c.) shows limited inhibitory effect on K. pneumoniae SHV-5-induced sepsis in mice, with an ED₅₀ >40 mg/kg, but it can enhance the efficacy of Ceftazidime when administered in combination^[1].

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

Animal Model:

ICR mice (male, 20-22 g, intraperitoneal inoculation with S. aureus 3816)^[1]
Dosage:

2.6 mg/kg (alone); 1.2 mg/kg (4:1 CAZ:AM-112 combination); 1 mg/kg (7:1 CAZ:AM-112 combination)
Administration:

subcutaneous injection
Result:

Had an ED₅₀ of 2.6 mg/kg (95% CI: 2.2-3.1 mg/kg).
Had an ED₅₀ of 1.2 mg/kg (95% CI for co-administered ceftazidime: 4.0-5.8 mg/kg) in 4:1 CAZ:AM-112 combination.
Had an ED₅₀ of 1 mg/kg (95% CI for co-administered ceftazidime: 6.6-9.7 mg/kg) in 7:1 CAZ:AM-112 combination.

Animal Model:

CD1 mice (male, 20-22 g, intraperitoneal inoculation with E. cloacae P99)^[1]
Dosage:

19 mg/kg (alone); 2 mg/kg (1:1 CAZ:AM-112 combination); 1.9 mg/kg (2:1 CAZ:AM-112 combination); 2.9 mg/kg (4:1 CAZ:AM-112 combination)
Administration:

intravenous injection
Result:

Had an ED₅₀ of 19 mg/kg (95% CI: 11.6-33.4 mg/kg).
Had an ED₅₀ of 2 mg/kg (95% CI for co-administered ceftazidime: 1.0-5.5 mg/kg) in 1:1 CAZ:AM-112 combination.
Had an ED₅₀ of 1.9 mg/kg (95% CI for co-administered ceftazidime: 2.3-5.9 mg/kg) in 2:1 CAZ:AM-112 combination.
Had an ED₅₀ of 2.9 mg/kg (95% CI for co-administered ceftazidime: 7.2-17.4 mg/kg) in 4:1 CAZ:AM-112 combination.

Animal Model:

ICR mice (female, 20-22 g, intraperitoneal inoculation with K. pneumoniae SHV-5)^[1]
Dosage:

>40 mg/kg (alone); 33.6 mg/kg (1:1 CAZ:AM-112 combination); 11.9 mg/kg (2:1 CAZ:AM-112 combination)
Administration:

subcutaneous injection
Result:

Had an ED₅₀ of >40 mg/kg (no 95% CI determined).
Had an ED₅₀ of 33.6 mg/kg (95% CI for co-administered ceftazidime: 25.1-45.1 mg/kg) in 1:1 CAZ:AM-112 combination.
Had an ED₅₀ of 11.9 mg/kg (95% CI for co-administered ceftazidime: 18.8-30.1 mg/kg) in 2:1 CAZ:AM-112 combination.

Chemical Information

CAS. Nr. 414858-51-8
Molecular Weight 298.34
Formel C₁₄H₂₂N₂O₅
SMILES

[C@H](C)(O)[C@@]1([C@@]2(N(C(C(O)=O)=C(C(CCCN)(C)C)O2)C1=O)[H])[H]
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]. Simpson IN, et al. Synthesis and biological activity of AM-112 and related oxapenem analogues. J Antibiot (Tokyo). 2003;56(10):838-847. [Content Brief]

[2]. Jamieson CE, et al. In vitro activities of novel oxapenems, alone and in combination with ceftazidime, against gram-positive and gram-negative organisms. Antimicrob Agents Chemother. 2003;47(8):2615-2618. [Content Brief]

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

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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AM-112

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