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Luffariellolide
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。
Luffariellolide图片
CAS NO:111149-87-2
包装:1mg
市场价:2310元

产品介绍
Luffariellolide 是人类滑液磷脂酶 A2 (HSF-PLA2) 的抑制剂 (IC50=5 μM)。
Cas No.111149-87-2
化学名4-[(3E,7E)-4,8-dimethyl-10-(2,6,6-trimethyl-1-cyclohexen-1-yl)-3,7-decadien-1-yl]-5-hydroxy-2(5H)-furanone
Canonical SMILESCC1(C)CCCC(C)=C1CC/C(C)=C/CC/C(C)=C/CCC2=CC(OC2O)=O
分子式C25H38O3
分子量386.6
溶解度Soluble in ethanol;Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Luffariellolide is an agonist for the RA receptors RAR α, β, and γ.

Retinoids show anti-tumour activity on various cancer cells and thus have been used as important therapeutic agents. However, adverse side effects and retinoic acid (RA) resistance limit its further development.

In vitro: Previous study reported the identification of luffariellolide, a natural marine product activating RA receptors (RARs) with a chemical structure distinct from retinoids by high-throughput screening. Luffariellolide was found to be a novel RAR agonist via inducing co-activator binding to RA receptors, further inhibiting cell growth and regulating RAR target genes in various cancer cells [1].

In vivo: In a previous animal study, paw edema was produced in CD-1 mice by the injection snake venom PLA2 into the hind paw. It was found that luffariellolide and aristolochic acid could reduce the edema but only when coinjected with the PLA2. Similarly, the PAF antagonists, CV-6202 and kadsurenone (coinjected) were also able to reduce the PLA2-induced edema, and high doses of the corticosteroids, dexamethasone and hydrocortisone were also effective [2].

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

References:
[1] Wang S, Wang Z, Lin S, Zheng W, Wang R, Jin S, Chen J, Jin L, Li Y.  Revealing a natural marine product as a novel agonist for retinoic acid receptors with a unique binding mode and inhibitory effects on cancer cells. Biochem J. 2012 Aug 15;446(1):79-87.
[2] Calhoun, W. ,Yu, J.,Sung, A., et al. Pharmacologic modulation of D-49 phospholipase A2-induced paw edema in the mouse. Agents and Actions 27, 418-421 (1989).