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  3. Piericidin A

Piericidin A (Synonyms: AR-054)

目录号: HY-114936 纯度: ≥95.0%
产品使用指南

Piericidin A (AR-054) 是一种天然线粒体 NADH-泛醌氧化还原酶 (复合物 I; complex I) 抑制剂。Piericidin A 是一种有效的神经毒素,通过其对 NADH-泛醌还原酶 (NADH-ubiquinone reductase) 的作用破坏电子传输系统,从而抑制线粒体呼吸。Piericidin A 还是一种潜在的群体感应抑制剂,可抑制胡萝卜欧文氏菌亚种 atroseptica (Eca) 的毒力基因的表达。Piericidin A 是一种 ADC 细胞毒素,具有抗菌,抗癌,杀虫活性。

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Piericidin A Chemical Structure

Piericidin A Chemical Structure

CAS No. : 2738-64-9

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1 mg (12.03 mM * 200 μL in Ethanol) ¥4500 In-stock

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  • 生物活性

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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[1][2][2].

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[1].
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[3].

MCE 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[1].

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

分子量

415.57

Formula

C₂₅H₃₇NO₄

CAS 号
中文名称
SMILES

COC1=C(C(C)=C(N=C1OC)C/C=C(C/C=C/C(C)=C/[C@@H](C)[C@H](/C(C)=C/C)O)\C)O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Solution, -20°C, 2 years

参考文献

Purity: ≥95.0%

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× = ×
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Keywords:

Piericidin AAR-054AR054AR 054BacterialADC CytotoxinAntibioticTaumitochondrialcomplex Ilipophilictauopathiesanticanceranti-bacterialneurotoxinADCcytotoxinInhibitorinhibitorinhibit

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Piericidin A
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