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Piericidin A
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。
Piericidin A图片
CAS NO:2738-64-9
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 AppearanceA solution in ethanol
StorageStore at -80°C
M.Wt415.6
Cas No.2738-64-9
FormulaC25H37NO4
SynonymsAR 054|Shaoguanmycin B|SN 198E
SolubilitySoluble in DMSO
Chemical Name2-[(2E,5E,7E,11E)-10R-hydroxy-3,7,9R,11-tetramethyl-2,5,7,11-tridecatetraen-1-yl]-5,6-dimethoxy-3-methyl-4-pyridinol
Canonical SMILESCOC1=C(O)C(C)=C(C/C=C(C)/C/C=C/C(C)=C/[C@H]([C@@H](O)/C(C)=C/C)C)N=C1OC
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

Piericidin A is a mitochondrial complex I inhibitor.

Complex I, also known as NADH:ubiquinone oxidoreductase, catalyzes the transfer of electrons from NADH to ubiquinone as part of the respiratory chain resulting in ATP generation.

In vitro: Previous study found that piericidin A could inhibit the electron transport system at two sites. Piericidin A specifically reacted at very low concentrations at a site near the reduced NADH dehydrogenase. At high concentrations, piericidin A inhibited the succinic dehydrogenase system, and the inhibition could be partially reversed by coenzyme Q. Moreover, it was found that both the succinate and NADH oxidase system were inhibited at high levels of piericidin A [1].

In vivo: Animal study was performed to evaluate the effect of piericidin A and antagonistic effect of vitamin K3 on respiration, blood pressure and heart rate in rats. Results showed that 0.167 mg/kg of piericidin A increased the respiratory rate and the lowered blood pressure rapidly. Furthermore, vitamin K3 (10-40 mg/kg) could restore the responses to piericidin A in rats [2].

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

References:
[1] Jeng M, Hall C, Crane FL, Takahashi N, Tamura S, Folkers K.  Inhibition of mitochondrial electron transport by piericidin A and related compounds. Biochemistry. 1968 Apr;7(4):1311-22.
[2] Mitsui T et al.  Studies on piericidin antagonistic effect of vitamin K3 on the respiratory chain of insects and mammals in the presence of piericidin A. Agricultural and Biological Chemistry Vol. 34 (1970) No. 7 P 1101-1109

试验操作

Cell experiment:[1]

Cell lines

Lepidopteran Tn5B1-4 cells, as well as human HepG2 and Hek293 cells

Reaction Conditions

0.02, 0.04, 0.08, 0.16 and 0.32 μM piericidin A for Tn5B1-4 cells; 180, 210, 240, 270 and 300 μM for HepG2 and Hek293 cells; for 48 h incubation

Applications

Piericidin A inhibited the viability of Tn5B1-4 cells in a time- and concentration-dependent manner with an IC50 value of 0.061 μM, whilst piericidin A showed slight inhibitory effect on the viability of HepG2 and Hek293 cells with IC50 values of 233.97 μM and 228.96 μM, respectively. Piericidin A-induced apoptosis of Tn5B1-4 cells coincided with a decrease in the mitochondrial membrane potential.

Animal experiment:[2]

Animal models

Male rats weighing 300 to 370 g

Dosage form

0.167 mg/kg

Administered through femoral vein

Applications

Piericidin A at the dose of 0.167 mg/kg substantially increased the respiratory rate and rapidly lowered the blood pressure in rats, which could be reversed by vitamin K3(10 ~ 40 mg/kg).

Note

The technical data provided above is for reference only.

References:

1. Muhayimana S, Zhang X, Xu J, et al. Cytotoxic selectivity and apoptosis induction of piericidin A contributes potentially to its insecticidal effect against Mythimna separata (Lepidoptera: Noctuidae) larvae. Pesticide Biochemistry and Physiology, 2019, 157: 19-25.

2. Mitsui T, Fukami J, Fukunaga K, et al. Studies on piericidin antagonistic effect of vitamin K3 on the respiratory chain of insects and mammals in the presence of piericidin A. Agricultural and Biological Chemistry, 1970, 34(7): 1101-1109.