A-54556A

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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。

CAS NO:

95398-45-1

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	718.9
Cas No.	95398-45-1
Formula	C₃₈H₅₀N₆O₈
Synonyms	ADEP 1,A-54556 Factor A
Solubility	Soluble in DMSO
Chemical Name	(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 SMILES	O=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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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).

试验操作

细胞实验 [1]：
细胞系	枯草芽孢杆菌
溶解方法	在DMSO中是可溶的。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。
反应条件	1.6 mg/ml
应用	先前的研究发现，用1.6 mg / ml的A-54556A处理枯草芽孢杆菌可使活细胞数量减少2个对数单位。用2 mg / ml A-54556A处理一个小时，DNA，RNA，蛋白质，细胞壁和脂肪酸的生物合成不受影响，而传统抗生素通过优先抑制其靶向途径而有明显区别。
动物实验 [1]：
动物模型	细菌感染的小鼠
剂量	1 mg / kg ADEP 2或0.5 mg / kg ADEP 4
应用	研究结果表明，A-54556A的两个类似物ADEP 2和ADEP 4在啮齿类动物的细菌感染治疗中具有活性。当小鼠受到致死性大肠埃希菌全身性感染攻击时，用1 mg / kg ADEP 2或0.5 mg / kg ADEP 4处理，小鼠得以100％存活。
注意事项	请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。
References: [1]. Brotz-Oesterhelt H, Beyer D, Kroll HP, Endermann R, Ladel C, Schroeder W, Hinzen B, Raddatz S, Paulsen H, Henninger K, Bandow JE, Sahl HG, Labischinski H. Dysregulation of bacterial proteolytic machinery by a new class of antibiotics.Nat Med. 2005 Oct;11(10):1082-7. Epub 2005 Oct 2. Erratum in: Nat Med. 2005 Dec;11(12):1361. PubMed PMID: 16200071.