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Arachidonic Acid Leelamide
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。
Arachidonic Acid Leelamide图片
规格:98%
分子量:571.9
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
phospholipase A2 inhibitor
货号:ajcx11436
CAS:
分子式:C40H61NO
分子量:571.9
溶解度:≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Arachidonic acid leelamide is a phospholipase A2 inhibitor.

Phospholipase A is a hydrolase responsible for the release of arachidonic acid from the sn2 position of phospholipids. The released arachidonic acid is then converted to mediators of inflammation by the enzymes prostaglandin synthetase and 5lipoxygenase, respectively. The inhibition of phospholipase A leads to a decrease in the release of arachidonic acid and, consequently, the inflammatory mediators.

In vitro: Arachidonic acid leelamide is the arachidonic amide analog of leelamine with no published pharmacological properties. For leelamine, it was found that electron micrographs of leelamine-treated cancer cells had accumulation of autophagosomes, membrane whorls, and lipofuscin-like structures. In addition, leelamine-mediated killing was a caspase-independent event triggered by cholesterol accumulation in the early process [1].

In vivo: In a previous study, authors identified the inductive effect of leelamine on CYP2B at doses of 5, 10, or 20 mg/kg in male ICR mice for 1 or 3 days. It was found that in liver, the activity of CYP2B significantly increased 3.6-fold after leelamine treatment. Activities of benzyloxyresorufin O-dealkylase and pentoxyresorufin O-dealkylase significantly increased 6.3- and 5.3-fold, respectively, with a single treatment of 20 mg/kg leelamine. Moreover, immunoblot analyses showed that significantly and dose-dependently increased CYP2B10 protein levels in liver. However, PCR results demonstrated that there were no significant changes in the CAR and CYP2B mRNA levels after leelamine treatment [2].

Clinical trial: So far, no clinical study has been conducted.

参考文献:
[1] Kuzu OF, Gowda R, Sharma A, Robertson GP.  Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport. Mol Cancer Ther. 2014 Jul;13(7):1690-703.
[2] Sim J, Nam W, Lee D, Lee S, O H, Joo J, Liu KH, Han JY, Ki SH, Jeong TC, Lee T, Lee S.  Selective induction of hepatic cytochrome P450 2B activity by leelamine in vivo, as a potent novel inducer. Arch Pharm Res. 2015;38(5):725-33.