MedChemExpress - Model AACOCF3 - 149301-79-1
AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease[1][2][3].MCE products for research use only. We do not sell to patients.
AACOCF3
MCE China：AACOCF3
Brand：MedChemExpress (MCE)
Cat. No.HY-108611
CAS：149301-79-1
Synonyms：Arachidonyl trifluoromethyl ketone
Purity：99.0%
Storage：Solution, -20°C, 2 years
Shipping：Room temperature in continental US; may vary elsewhere.
Description：AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease.
In Vitro：AACOCF3 inhibits the release of arachidonic acid from calcium ionophore-challenged U937 cells (IC50= 8 μM, 2 x 106 cells ml-1) and from platelets (IC50= 2 μM, 4 x 107 cells ml-1)[1]. AACOCF3 (10 μM) suppresses phosphate-induced calcification and osteogenic/chondrogenic signaling in HAoSMCs. AACOCF3 significantly inhibits both basal and Pi-induced release of arachidonic acid, the product of PLA2 activity[2].
In Vivo：AACOCF3 (10 mg/kg; gavage; 5 days a week; ApoE–/– mice (6-week-old males) were fed a high-cholesterol diet) significantly reduces type III collagen plaque expression but had no significant influence on total collagen accumulation[3].
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References：
[1]. Riendeau D, 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. [Content Brief]
[2]. Schanstra JP, et al. Systems biology identifies cytosolic PLA2 as a target in vascular calcification treatment. JCI Insight. 2019;4(10):e125638. Published 2019 May 16. [Content Brief]
[3]. Loweth AC, et al. A specific inhibitor of cytosolic phospholipase A2 activity, AACOCF3, inhibits glucose-induced insulin secretion from isolated rat islets. Biochem Biophys Res Commun. 1996;218(2):423-427. [Content Brief]
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