Palmitoylethanolamide

製品コードS4708 バッチS470802

印刷

化学情報

 Chemical Structure Synonyms Palmidrol|N-palmitoylethanolamine Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C18H37NO2

分子量 299.49 CAS No. 544-31-0
Solubility (25°C)* 体外 Ethanol 16 mg/mL (53.42 mM)
DMSO 3 mg/mL (10.01 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.
in vitro PEA protects cultured mouse cerebellar granule cells from glutamate toxicity and enhances microglial cell motility. In the mitochondrial fraction from cells stimulated with PEA, steroidogenic acute regulatory protein (StAR) and cytochrome P450 enzyme(P450scc) expression increases, both comprising proteins considered to be involved in crucial steps of neurosteroid formation. Moreover, PEA shows a protective effect, reducing malondialdehyde formation in cells treated with L-buthionine-(S,R)-sulfoximine, a glutathione depletor and the effect of PEA is partially inhibited by finasteride, a 5a-reductase inhibitor[2].
in vivo PEA attenuates inflammation in wild-type mice but has no effect in mice deficient in PPAR-α. PEA has been shown to inhibit peripheral inflammation and mast-cell degranulation as well as to exert neuroprotective and antinociceptive effects in rats and mice. These actions are accompanied by changes in nitric oxide production, neutrophil influx, and expression of proinflammatory proteins such as inducible nitric oxide synthase and cyclooxygenase-2[1]. In addition to its known anti-inflammatory activity, PEA regulates many pathophysiological processes, including pain perception, convulsions, and neurotoxicity. In the central nervous system (CNS), where PEA is present at detectable levels, its concentrations significantly increase under pathological conditions, such as excitotoxicity, brain ischaemia and neuroinflammation[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Rat C6 glioma cells
濃度 10 μM
反応時間 24 h
実験の流れ C6 glioma cells (300 000⁄P60 dish) or astrocyte primary culture are incubated in serum-free DMEM at 37℃ for at least 24 h before each experiment. Then, cells are treated with PEA (10 μM) for 24 h in serum-free medium, in the presence and absence of GW6471 (10 μM) added 30 min before ethanolamide treatment. The concentration of PEA is chosen on the basis of preliminary experiments, assessing drug efficacy without modifi-cation of cell viability. PEA and GW6471 are first dissolved in absolute ethanol and then diluted with DMEM. The final ethanol concentration was< 0.5%. Mitochondrial protein extracts from C6 or astrocytes are obtained. Alternatively after 24 h of starvation in serum-free DMEM, C6 cells are treated with FIN (100 nM). After 30 min, PEA (10 μM) and⁄or ALLO (3 μM) is added and, 30 min later, are stimulated with BSO (10 mM). After 18 h, MDA is evaluated. In this set of experiments, FIN and⁄or PEA are dissolved in dimethylsulphoxide (DMSO) and then diluted with DMEM (0.1% final DMSO concentration).
動物実験 動物モデル C57BL6 mice, male C57BL6 PPAR-α-/- mice
投薬量 10 mg/kg
投与方法 i.p

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Effects of Tacrolimus and Other Immune Targeting Compounds on Binge-Like Ethanol Drinking in High Drinking in the Dark Mice [ Neurosci Insights, 2020, 15:2633105520975412] PubMed: 33294845
SIRT2 plays a novel role on progesterone, estradiol and testosterone synthesis via PPARs/LXRα pathways in bovine ovarian granular cells [Xu D, et al. J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005] PubMed: 30009951

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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