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A-54556A

An acyldepsipeptide antibiotic

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A-54556A的二维码
  • 库存: 现货
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  • 1mg
    ¥5737.00
    4590.00
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  • 5mg
    ¥19887.00
    15910.00
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  • 货号: ajci10086
  • CAS: 95398-45-1
  • 别名: ADEP 1,A-54556 Factor A
  • 分子式: C38H50N6O8
  • 分子量: 718.9
  • 纯度: >98%
  • 溶解度: DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble
  • 储存: Store at -20°C
  • 库存: 现货

Background

IC50: 0.2 μg/ml for Bacillus subtilis 168


A-54556A is a natural acyldepsipeptide (ADEP) antibiotic.


Acyldepsipeptides (ADEP), a new class of antibiotics, has antibacterial activity against Gram-positive bacteria. The acyldepsipeptides are active against isolates that are resistant to antibiotics, implying a new target identify as ClpP.


In vitro: Previous study found that the treatment of B. subtilis with 1.6 mg/ml of A-54556A reduced the number of viable cells by 2 log units. In addition, the biosynthesis of DNA, RNA, protein, cell wall and fatty acid proceeded unhindered for 1 h at 2 mg/ml A-54556A, whereas classical antibiotics were clearly distinguished by preferential inhibition of their target pathway. Microscopic examination showed that after addition of A-54556A at concentrations as low as 0.4 mg/ml, B. subtilis started to form filaments [1].


In vivo: Two A-54556A analogs, ADEP 2 and ADEP 4, were proven to be active in the treatment of bacterial infections in rodents. When mice were challenged with a lethal systemic infection of E. faecalis, 1 mg/kg ADEP 2 or 0.5 mg/kg ADEP 4 were sufficient for 100% survival. In lethal sepsis caused by S. aureus, 12.5 mg/kg ADEP 4 rescued 80% of the mice and reduced the bacterial loads in liver, spleen and lung by 2–3 log units compared to an untreated control [1].


Clinical trial: Up to now, A-54556A is still in the preclinical development stage.

Reference:
[1] H.? Brtz-Oesterhelt, D. Beyer, H. P. Kroll, et al. Dysregulation of bacterial proteolytic machinery by a new class of antibiotics. Nature Medicine 11(10), 1082-1087 (2005).

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