Apramycin (Nebramycin II)
(Synonyms: 安普霉素) 目录号 : GC32288
Apramycin (Nebramycin II)是一种动物用氨基糖苷类抗生素，广泛用于治疗沙门氏菌、大肠杆菌和其他感染。
Cas No.:37321-09-8
Sample solution is provided at 25 µL, 10mM.
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Apramycin (Nebramycin II), an aminoglycoside antibiotic for animals, is widely used to treat Salmonella, Escherichia coli, and other infections[1]. Apramycin showed potent in-vitro activity against hypervirulent carbapenem-resistant K pneumoniae isolates, including those resistant to amikacin or gentamicin[2].
Apramycin (50mg/L, overnight) was used as a selection marker to successfully select isolates with the restoration of functional wild type Ompk35 or Ompk36[3].
Apramycin (20mg/kg, i.p.) and citrulline combined with glutamine significantly improved the body condition of the infected mice[1]. Apramycin (20, 80, or 500mg/kg, s.c.) demonstrated a dramatic therapeutic effect against A. baumannii strains MSRN7465, MSRN1450 and FDA-CDC278 in neutropenic murine thigh infection model[4].
References:
[1] Yong Y, Zhou Y, Liu K, et al. Exogenous citrulline and glutamine contribute to reverse the resistance of Salmonella to apramycin. Frontiers in Microbiology. 2021 Oct 14;12:759170.
[2] Melchiorri D, Rocke T, Alm RA, et al. Addressing urgent priorities in antibiotic development: insights from WHO 2023 antibacterial clinical pipeline analyses. The Lancet Microbe. 2024 Oct 22.
[3] Sun L, Li H, Wang Q, et al. Increased gene expression and copy number of mutated bla KPC lead to high-level ceftazidime/avibactam resistance in Klebsiella pneumoniae. BMC microbiology. 2021 Dec;21:1-0.
[4] Kang AD, Smith KP, Berg AH, et al. Efficacy of apramycin against multidrug-resistant Acinetobacter baumannii in the murine neutropenic thigh model. Antimicrobial agents and chemotherapy. 2018 Apr;62(4):10-128.
Apramycin (Nebramycin II)是一种动物用氨基糖苷类抗生素，广泛用于治疗沙门氏菌、大肠杆菌和其他感染[1]。Apramycin对高毒力的耐卡巴培南肺炎克雷伯菌分离株（包括对阿米卡星或庆大霉素有耐药性的分离株）表现出强效的体外活性[2]。
Apramycin（50mg/L，过夜）被用作选择标记，成功筛选出恢复功能性野生型Ompk35或Ompk36的分离株[3]。
Apramycin（20mg/kg，腹腔注射）和瓜氨酸与谷氨酰胺联合使用可显著改善受感染小鼠的身体状况[1]。Apramycin（20、80或500mg/kg，皮下注射）在粒细胞减少性小鼠大腿感染模型中对鲍曼不动杆菌菌株MSRN7465、MSRN1450和FDA-CDC278表现出显著的治疗效果[4]。
| Cell experiment [1]: | |
Cell lines | The competent cells of Klebsiella pneumoniae clinical isolates |
Preparation Method | The competent cells of Klebsiella pneumoniae clinical isolates were prepared using 10% glycerol. The mixture of 50μl electrocompetent cells and 5μl plasmid was transferred into a 2mm electroporation cuvette and electroporated using MicroPuler System (Bio-Rad) at 2.5kV. The cells were plated onto Luria-Bertani (LB) agar containing Apramycin at 50mg/L. The plates were incubated at 37°C overnight, and the successful clone was identified using PCR and sequencing. PCR detection for the presence of beta-lactamase genes encoding carbapenemases, ESBL associated genes, and plasmid-borne AmpC beta-lactamases were performed. Outer membrane protein genes were amplified by PCR. PCR amplicons were sequenced and compared with sequences available in the GenBank database using BLAST searches. |
Reaction Conditions | 50mg/L, overnight |
Applications | Apramycin was used as a selection marker to successfully select isolates with the restoration of functional wild type Ompk35 or Ompk36. |
| Animal experiment [2]: | |
Animal models | Neutropenia mouse Apramycin-resistant Salmonella strains infection model |
Preparation Method | Ninety healthy female mice were divided into nine groups, with 10 mice in each group. The groups comprised the negative control group without bacterial infection, the positive control group (mice infected with drug-resistant bacteria but without any treatment), and the other seven groups were treated with Apramycin, citrulline, glutamine, Apramycin plus citrulline, Apramycin plus glutamine, or Apramycin plus citrulline plus glutamine, respectively, after infection with drug-resistant bacteria. All animals were tested and found to be Salmonella typhimurium-free before the start of experiments. Eighty mice were intraperitoneally injected with cyclophosphamide for 5 days to establish a neutropenia model. After the establishment of the model, 0.1ml Apramycin-induced Salmonella typhimurium (Apr-R-CICC21484) suspension was injected intraperitoneally at a concentration of 107 colony-forming units/ml. At 12h after infection, the mice in the experimental group were injected intraperitoneally with Apramycin or citrulline and glutamine. The doses of Apramycin, citrulline, and glutamine used in the experiment were 20mg/kg body weight (b.w.), 240mg/kg b.w., and 200mg/kg b.w., respectively. At 24h after treatment, all mice were euthanized. The liver, spleen, and blood of all mice were collected under sterile conditions and placed in saline. The tissue or blood of each mouse was homogenized separately, diluted with saline, and inoculated on different nutrient agar plates. Finally, the bacterial load of each mouse liver, spleen, and a blood sample was calculated to evaluate the effect of different treatment schemes. |
Dosage form | 20mg/kg, i.p. |
Applications | Apramycin and citrulline combined with glutamine significantly improved the body condition of the infected mice. |
References: | |
| Cas No. | 37321-09-8 | SDF | |
| 别名 | 安普霉素 | ||
| Canonical SMILES | O[C@H]1[C@](O[C@H](O[C@@]([C@H](C[C@H]2N)N)([H])[C@@H]([C@H]2O)O)[C@H](N)C3)([H])[C@@]3([H])O[C@H](O[C@@]([C@@H]([C@@H](O)[C@@H]4N)O)([H])O[C@@H]4CO)[C@H]1NC | ||
| 分子式 | C21H41N5O11 | 分子量 | 539.58 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8533 mL | 9.2665 mL | 18.5329 mL |
| 5 mM | 0.3707 mL | 1.8533 mL | 3.7066 mL |
| 10 mM | 0.1853 mL | 0.9266 mL | 1.8533 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >95.00%
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