Drug intelligence / Profile preview

arachidonyl trifluoromethyl ketone

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Arachidonyl trifluoromethyl ketone (AACOCF3) is a synthetic analog of arachidonic acid in which the carboxylic acid group is replaced by a trifluoromethyl ketone. It acts as a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2), particularly the 85 kDa isoform. By irreversibly alkylating the enzyme's active site, it blocks the release of arachidonic acid from membrane phospholipids and thereby inhibits downstream production of pro-inflammatory eicosanoids such as prostaglandins and leukotrienes. AACOCF3 also inhibits other enzymes involved in eicosanoid biosynthesis including cyclooxygenases (COX) and lipoxygenases to some extent[1][2][3][5]. It has been widely used as a research tool to study inflammatory pathways and neuroinflammation; it has shown neuroprotective effects in animal models of spinal cord injury and multiple sclerosis[2][5]. There is no evidence that it is approved for clinical use; its applications are limited to laboratory research.

Other names
arachidonyltrifluoromethane1,1,1-trifluoro-6Z,9Z,12Z,15Z-heneicosatetraen-2-onearachidonic acid trifluoromethyl ketone
02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)PLA2 (Phospholipase A2 group IID)

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