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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
规格:98%
分子量:356.47
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍

Inhibitor of cPLA2/anandamide hydrolysis/FAAH
CAS:149301-79-1
分子式:C21H31F3O
分子量:356.47
纯度:98%
存储:Store at -20°C

Background:

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].

参考文献:
[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.