2. Anti-infection
  3. Antibiotic Beta-lactamase Bacterial Penicillin-binding protein (PBP)
  4. AM-112

AM-112 是一种 β-内酰胺酶 (β-lactamase) 抑制剂与抗菌剂，针对 A 类、C 类和 D 类 β-lactamase 的 IC50 为 0.0002 μg/mL-0.67 μg/mL。AM-112 通过抑制大肠杆菌的青霉素结合蛋白 PBP2 并保护 Ceftazidime (HY-B0593) 免受酶解水解，显著增强了 Ceftazidime 对革兰氏阴性菌、肠球菌及葡萄球菌的抗菌效力。AM-112 具有良好药代动力学特性和酸碱稳定性。AM-112 可用于细菌感染的研究。

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AM-112

AM-112 Chemical Structure

CAS No. : 414858-51-8

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AM-112 相关抗体

Top Publications Citing Use of Products

查看 Antibiotic 亚型特异性产品:

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

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Metallo-β-lactamase (MBL) Serine β-lactamase (SBL)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2].

IC50 & Target

β-lactam

 

体外研究
(In Vitro)

AM-112 (与 Ceftazidime 以 2:1 比例组合) 可在所有受试粪肠球菌菌株中协同降低 Ceftazidime (HY-B0593) 的 MIC，其中对 E. faecalis SFZ 的 MIC 降幅最大 (从 64 μg/mL 降至 8 μg/mL)[1]。
AM-112 (0.5-32 μg/ml；18-24 h) 单独使用时对 Methicillin (HY-121544) 敏感金黄色葡萄球菌的 MIC 为 2 μg/ml，对梭菌属、拟杆菌属厌氧菌的 MIC 范围为 4-16μg/ml，对大肠杆菌、假单胞菌、不动杆菌、肠球菌及耐甲氧西林金黄色葡萄球菌的 MIC 均≥32μg/ml[2]。

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

AM-112 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

AM-112 (皮下注射，1-2.6 mg/kg) 对金黄色葡萄球菌诱导的小鼠脓毒症表现出强抑制活性，其 ED50 为 2.6 mg/kg，且与 Ceftazidime (HY-B0593) 联用时可增强后者的药效[1]。
AM-112 (静脉注射，1.9-19 mg/kg) 对 E. cloacae P99 诱导的小鼠败血症具有抑制作用，ED50 为 19 mg/kg，且联合给药时可显著增强 Ceftazidime 的药效[1]。
AM-112 (>40 mg/kg; 皮下注射) 对 K. pneumoniae SHV-5 诱导的小鼠败血症的抑制效果有限，其 ED50 >40 mg/kg，但联合给药时可增强 Ceftazidime 的效果[1]。

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.
分子量

298.34

Formula

C14H22N2O5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AM-112 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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:

AM-112414858-51-8AM112AM 112AntibioticBeta-lactamaseBacterialPenicillin-binding protein (PBP)β-lactamaseClass D β-lactamasesβ-lactamase inhibitorClass C β-lactamasesClass A β-lactamasesEscherichia coliStaphylococcus aureuspenicillin-binding protein 2bacterial infectionEnterococcus faecalisGram-negative bacteriaInhibitorinhibitorinhibit

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