Amikacin hydrate

目录号: GC15685纯度: >98%同义词: 阿米卡星水合物
Amikacin hydrate是一种氨基糖苷类抗生素。Amikacin hydrate被应用于治疗多种由革兰氏阴性菌引起的感染。

Amikacin hydrate
Cas No.: 1257517-67-1
规格价格库存数量操作
50mg¥350.00现货
1
100mg¥560.00现货
1

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产品描述 Description

Amikacin hydrate is an aminoglycoside antibiotic[1]. Amikacin hydrate is used to treat a variety of infections caused by Gram-negative bacteria[2]. Amikacin hydrate can enter bacterial cells and bind to their ribosomes. By interfering with bacterial protein synthesis, it prevents normal bacterial growth and reproduction, thereby exerting its antibacterial effects [3]. Amikacin hydrate is widely used in the treatment of complex urinary tract infections, respiratory infections, and sepsis[4].

In vitro, Amikacin hydrate (0.003 - 25mg/mL) treatment of equine joint cells (including chondrocytes, synovial cells, adipose-derived and bone marrow-derived mesenchymal stem cells) induces rapid cell death within 1 hour in a dose-dependent manner. Moreover, the cytotoxicity of Amikacin hydrate is not mitigated by the presence of synovial fluid[5]. Amikacin hydrate (32mg/L) alone or in combination with 2mg/L Colistin can effectively kill bacteria within biofilms of mature Pseudomonas aeruginosa (PAO1 and CRPAO1) treatment for 24 hours[6].

In vivo, Amikacin hydrate (15mg/kg) combined with Imipenem (40mg/kg) administered intraperitoneally every 8 hours is used to treat mice infected with drug-resistant Escherichia coli. The combination of Amikacin hydrate and Imipenem significantly reduces the bacterial count in the blood of mice[7]. Amikacin hydrate (7.5mg/kg; every 12 hours) combined with Meropenem (200mg/kg; every 8 hours) administered intraperitoneally to mice infected with carbapenem-resistant Enterobacteriaceae (CRE). Compared to Meropenem monotherapy, the combination therapy significantly reduces bacterial density in the thigh muscles of mice and increases survival rates[8].

References:
[1] Ramirez MS, Tolmasky ME. Amikacin hydrate: Uses, Resistance, and Prospects for Inhibition. Molecules. 2017 Dec 19;22(12):2267.
[2] Meyer RD. Amikacin hydrate. Ann Intern Med. 1981 Sep;95(3):328-32.
[3] Jenkins A, Thomson AH, Brown NM, et al. Amikacin hydrate use and therapeutic drug monitoring in adults: do dose regimens and drug exposures affect either outcome or adverse events? A systematic review. J Antimicrob Chemother. 2016 Oct;71(10):2754-9.
[4] Kato H, Hamada Y. Amikacin hydrate Therapy in Japanese Pediatric Patients: Narrative Review. Int J Environ Res Public Health. 2022 Feb 10;19(4):1972.
[5] Pezzanite L, Chow L, Soontararak S, et al. Amikacin hydrate induces rapid dose-dependent apoptotic cell death in equine chondrocytes and synovial cells in vitro. Equine Vet J. 2020 Sep;52(5):715-724.
[6] Wang Y, Li C, Wang J, et al. The Efficacy of Colistin Combined with Amikacin hydrate or Levofloxacin against Pseudomonas aeruginosa Biofilm Infection. Microbiol Spectr. 2022 Oct 26;10(5):e0146822.
[7] Farhan SM, El-Baky RMA, Abdalla S, et al. In Vitro and In Vivo Effect of Amikacin hydrate and Imipenem Combinations against Multidrug-Resistant E. coli. Trop Med Infect Dis. 2022 Oct 2;7(10):281.
[8] Hagihara M, Kato H, Yamashita R, et al. In vivo study assessed meropenem and Amikacin hydrate combination therapy against carbapenem-resistant and carbapenemase-producing Enterobacteriaceae strains. J Infect Chemother. 2020 Jan;26(1):1-7.

Amikacin hydrate是一种氨基糖苷类抗生素[1]。Amikacin hydrate被应用于治疗多种由革兰氏阴性菌引起的感染[2]。Amikacin hydrate能够进入细菌细胞内,与细菌的核糖体结合。通过干扰细菌的蛋白质合成过程,阻止细菌正常生长和繁殖,从而发挥抗菌作用[3]。Amikacin hydrate常被用于治疗复杂性尿路感染、呼吸道感染以及败血症等疾病[4]

在体外,Amikacin hydrate(0.003 - 25mg/mL)处理马的关节细胞(包括软骨细胞、滑膜细胞、脂肪源性和骨髓源性间充质干细胞)1小时内,Amikacin hydrate快速诱导细胞死亡,且这种细胞毒性作用以Amikacin hydrate剂量依赖的方式发生。此外,Amikacin hydrate的细胞毒性作用不会因滑膜液的存在而减轻[5]。Amikacin hydrate(32mg/L)单独或与2mg/L的Colistin联合处理铜绿假单胞菌(PAO1和CRPAO1)生物膜24小时,能够有效杀灭生物膜内的细菌[6]

在体内,Amikacin hydrate(15mg/kg)联合Imipenem(40mg/kg)每8小时腹腔注射一次,用于处理感染耐药大肠杆菌的小鼠。Amikacin hydrate联合Imipenem显著减少了小鼠血液中的细菌数量[7]。Amikacin hydrate(7.5mg/kg;每12小时一次)联合Meropenem(200mg/kg;每8小时一次)腹腔注射处理感染了碳青霉烯类耐药肠杆菌科细菌(CRE)的小鼠。与单独使用Meropenem相比,联合治疗显著降低了小鼠大腿肌肉中的细菌密度,并提高了生存率[8]

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Equine chondrocytes, synovial cells, bone marrow-derived mesenchymal stem cells (BMD-MSC), and adipose-derived mesenchymal stem cells (AD-MSC).

Preparation Method

Cells were harvested from three donor horses and plated in triplicate wells for 48 hours prior to the addition of Amikacin hydrate(0.003 to 25mg/mL). Cells were maintained in complete DMEM media.

Reaction Conditions

0.003 to 25mg/mL; 12h

Applications

Amikacin hydrate induced rapid, dose-dependent cytotoxic effects on all cell types, primarily through apoptosis. Amikacin hydrate exposure decreased cellular metabolism and mitochondrial mass, and suppressed cell proliferation.

Animal experiment [2]:

Animal models

Neutropenic ICR Swiss mice

Preparation Method

Mice were intramuscularly inoculated with 10⁸cfu/mL of carbapenem-resistant Enterobacteriaceae (CRE) strains, followed by subcutaneous administration of Meropenem (200mg/kg every 8 hours) and Amikacin hydrate (7.5mg/kg every 12 hours) either alone or in combination.

Dosage form

7.5mg/kg; s.c.

Applications

The combination therapy of Meropenem and Amikacin hydrate significantly reduced bacterial density in the thigh muscles and increased survival rates compared to Meropenem monotherapy.

References:
[1] Pezzanite L, Chow L, Soontararak S, et al. Amikacin hydrate induces rapid dose-dependent apoptotic cell death in equine chondrocytes and synovial cells in vitro. Equine Vet J. 2020 Sep;52(5):715-724.
[2] Hagihara M, Kato H, Yamashita R, et al. In vivo study assessed meropenem and Amikacin hydrate combination therapy against carbapenem-resistant and carbapenemase-producing Enterobacteriaceae strains. J Infect Chemother. 2020 Jan;26(1):1-7.

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
1257517-67-1
同义词
阿米卡星水合物
化学名
(2S)-4-amino-N-[(1R,2S,3S,4R,5S)-5-amino-2-[(2S,3R,4S,5S,6R)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2R,3R,4S,5S,6R)-6-(aminomethyl)-3,4,5-trihydroxyoxan-2-yl]oxy-3-hydroxycyclohexyl]-2-hydroxybutanamide;hydrate
SMILES
C1C(C(C(C(C1NC(=O)C(CCN)O)OC2C(C(C(C(O2)CO)O)N)O)O)OC3C(C(C(C(O3)CN)O)O)O)N.O
分子式
C22H43N5O13.xH2O
分子量
585.6 g/mol
溶解性
100 mg/mL in Water (Need ultrasonic); 100 mg/mL in DMSO(Need ultrasonic);
保存条件
Store at -20°C
General tips
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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°C,然后在超声波浴中震荡一段时间。
Shipping Condition
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计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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