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Piericidin A (Synonyms: AR-054)
目录号: PC12715 纯度: ≥98%
CAS No. :2738-64-9
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中文名称
Piericidin A
中文别名
抗生素;杀粉蝶霉素A
英文名称
Piericidin A
英文别名
4-Pyridinol,2-[(2E,5E,7E,9R,10R,11E)-10-hydroxy-3,7,9,11-tetramethyl-2,5,7,11-tridecatetraen-1-yl]-5,6-dimethoxy-3-methyl-;PIERICIDIN A;2,6,9,11-Tridecatetraen-4-ol,13-(4-hydrox-5,6-dimethoxy-3-methyl-2-pyridyl)-3,5,7,11-tetramethyl-(all-E)-(4R,5R);4-Pyridinol,2-(10-hydroxy-3,7,9,11-tetramethyl-2,5,7,11-tridecatetraenyl)-5,6-dimethoxy- [R-[R*,R*-(all-E)]]-3-methyl-;Piericidin A1;SN 198E;Shaoguamycin B
Cas No.
2738-64-9
分子式
C25H37NO4
分子量
415.57
包装储存

Solution, -20°C, 2 years

生物活性

Piericidin A (AR-054) is a natural mitochondrial NADH-ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action on NADH-ubiquinone reductase. Piericidin A is also a potential quorum-sensing inhibitor that suppresses the expression of the virulence genes of Erwinia carotovora subsp. atroseptica (Eca). Piericidin A is an ADC cytotoxin and has anti-bacterial, anticancer, insecticidal activity.

性状

Liquid

体外研究(In Vitro)

In a cell free assay, the potency of Piericidin A to inhibit mitochondrial complex I is ~2 fold smaller than the one of annonacin. In cultured neurons, Piericidin A potently induces the redistribution of phosphorylated tau from the dendrites into the cell soma and induces cell death.
The viability of Tn5B1-4 cells is inhibited by Piericidin A in a time- and concentration-dependent manner with IC50 value of 0.061 μM, whilst Piericidin A shows slight inhibitory effect on the viability of HepG2 and Hek293 cells with IC50 value of 233.97 μM and 228.96 μM, respectively. Piericidin A induces apoptosis of Tn5B1-4 cells coincides with a decrease in the mitochondrial membrane potential.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Piericidin A (0.5 mg/kg/d; for 28 days via osmotic minipumps) significantly increases the number of phospho-tau immunoreactive cells in the cerebral cortex in P301S mice. Piericidin A leads to increased levels of pathologically phosphorylated tau only in P301S mice. The synaptic density is reduced by Piericidin A treatment in P301S mice. Exposure to Piericidin A aggravates the course of genetically determined tau pathology.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Solution, -20°C, 2 years

结构分类
来源

Streptomyces sp. BCC24731

参考文献
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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