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AACOCF3
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。
AACOCF3图片
CAS NO:149301-79-1
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍

AACOCF3 (Arachidonyl trifluoromethyl ketone) 是花生四烯酸的细胞渗透性三氟甲基酮类似物。

Cas No.149301-79-1
别名花生四烯基三氟甲酮,ATK, AATFMK
化学名1,1,1-trifluoro-6Z,9Z,12Z,15Z-heneicosatetraen-2-one
Canonical SMILESFC(F)(C(CCC/C=C\C/C=C\C/C=C\C/C=C\CCCCC)=O)F
分子式C21H31F3O
分子量356.47
溶解度DMF: >25 mg/ml,DMSO: >25 mg/ml,PBS pH 7.2:<50 µ g/ml
储存条件Store at -20℃, protect from light
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
文献引用
产品描述

AACOCF3 is a potent and selective inhibitor of cytosolic phospholipase A2 with IC50 value of 15 μM [1].

Phospholipase A2 is an enzyme that releases fatty acids from glycerol. Cytosolic phospholipase A2 (cPLA2) plays an important role in inflammation by inducing the release of arachidonic acid from membrane phospholipids.

AACOCF3 is a potent and selective inhibitor of the 85-kDa cPLA2. AACOCF3 inhibited macrophage PLA2 with IC50 value of 15 μM in a concentration-dependent way [1]. AACOCF3 inhibited the release of arachidonic acid (AA) with IC50 values of 2 and 8 μM in platelets and calcium ionophore-challenged U 937 cells, respectively. Also, AACOCF3 inhibited the production of thromboxane B and 12-hydroxyeicosatetraenoic acid (12-HETE), the major metabolites of AA in a dose-dependent way. These results suggested that cPLA2 played a critical role in the generation of AA and 12-HETE [2].

In mice, AACOCF3 inhibited chronic inflammatory responses and inhibited phorbol 12-myristate

13-acetate (PMA)-induced chronic ear edema. In ovalbumin-challenged BALB/c mice, AACOCF3 (20mg/kg) inhibited airway hyper-responsiveness and reduced cellular recruitment in the airway inflammation and airway lumen [3].

References:
[1]. Ackermann EJ, Conde-Frieboes K, Dennis EA. Inhibition of macrophage Ca(2+)-independent phospholipase A2 by bromoenol lactone and trifluoromethyl ketones. J Biol Chem, 1995, 270(1): 445-450.
[2]. Riendeau D, Guay J, Weech PK, et al. Arachidonyl trifluoromethyl ketone, a potent inhibitor of 85-kDa phospholipase A2, blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. J Biol Chem, 1994, 269(22): 15619-15624.
[3]. Malaviya R, Ansell J, Hall L, et al. Targeting cytosolic phospholipase A2 by arachidonyl trifluoromethyl ketone prevents chronic inflammation in mice. Eur J Pharmacol, 2006, 539(3): 195-204.