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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 414858-51-8
- 화학식: C14H22N2O5
- 분자량:298.34
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
|
β-lactam |
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 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.
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 No. 414858-51-8
-
분자량 298.34
-
화학식 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]
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AM-112 Related Classifications
HY-165460 Related Classifications
Powered by Bioz
- AM-112
- 414858-51-8
- AM112
- AM 112
- Antibiotic
- Beta-lactamase
- Bacterial
- Penicillin-binding protein (PBP)
- Class D β-lactamases
- β-lactamase inhibitor
- Class C β-lactamases
- Class A β-lactamases
- Escherichia coli
- Staphylococcus aureus
- penicillin-binding protein 2
- bacterial infection
- Enterococcus faecalis
- Gram-negative bacteria
- Inhibitor
- inhibitor
- inhibit