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A-54556A
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
A-54556A图片
CAS NO:95398-45-1
包装与价格：
包装价格(元)
1mg询价
5mg询价

natural acyldepsipeptide (ADEP) antibiotic
Cas No.95398-45-1
别名ADEP 1,A-54556 Factor A
化学名(4R)-(6→2)-lactone N-[(2E,4E,6E)-1-oxo-2,4,6-octatrien-1-yl]-L-phenylalanyl-L-seryl-L-prolyl-N-methyl-L-alanyl-L-alanyl-4-methyl-L-proline
Canonical SMILESO=C([C@@H](NC(/C=C/C=C/C=C/C)=O)CC1=CC=CC=C1)N[C@@H](COC2=O)C(N3[C@H](C(N([C@@H](C)C(N[C@H](C(N4[C@H]2C[C@@H](C)C4)=O)C)=O)C)=O)CCC3)=O
分子式C38H50N6O8
分子量718.9
溶解度DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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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