-
-
Overview
-
Please contact us at for specific academic pricing.
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].[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.
-
- Properties
- Reference
-
Overview
- Home
- Products
- Life Science
- Analytical Chromatography
- Assay Kits
- Biochemical Reagents
- Antibodies
- Antigens
- Enzymes
- Chemicals
- Proteins
- Liposomes
- Cell Culture
- Cell Analysis
- Cloning and Expression
- Nucleic Acid Synthesis
- Nucleic Acid Extraction
- Nucleic Acid Electrophoresis
- PCR
- Protein Gel Electrophoresis
- Protein Biochemistry
- Nanoparticles
- Glycan Analysis
- Immunohistochemistry (IHC)
- Microbiology
- Biospecimens
- Transfection Reagents
- Ion Exchange Resins
- Venoms
- Lab Solutions
- Lab Equipment
- Biosensors
- Flow Imaging Microscopes
- Fluorescence Quality Management Solutions
- Electrophoresis Systems
- Hematology Analyzers
- Isothermal Amplification Instruments
- Liquid Handling Equipment
- Luminometers
- Microfluidic Flow Control Systems
- Next-generation Sequencing Systems
- Nucleic Acid Purification Instruments
- Raman Spectroscopy Systems
- Sample Tracking Systems
- Spectrometer Accessories
- Syringe Pumps
- Thawing and Warming Systems
- Tissue Dissociation Systems
- Water Purification Systems
- Western Blotting Equipment
- General Laboratory Equipment
- Clinical Chemistry Analyzers
- Amerigo Scientific Instrument
- Automated Cell Selection Systems
- Automated Nucleic Acid Extraction Instruments
- Balances, Scales and Weighing
- Biolayer Interferometry Instruments
- Bioprocess Filtration Equipment
- Bioprocess Systems and Accessories
- Bioreactors and Fermenters
- Cappers and Decappers
- Cell Thawing Instruments
- Chromatography
- Data Loggers
- Droplet Generators
- Dry Baths
- Flow Cytometers
- Histology Laboratory Equipment
- Lab Ovens and Furnaces
- Lab Refrigeration Equipment
- Lab Shakers and Mixers
- Laboratory Centrifuges
- Laboratory Evaporators
- Laboratory Hoods
- Laboratory Incubators
- Laboratory Microscopes
- Laboratory Mills
- Laboratory Pumps
- Liquid Handling
- Live Cell Imaging Systems
- Microbiology Equipment
- Microscopy Flow Cells
- Mutation Breeding Instruments
- Oligonucleotide Synthesis Devices
- Particle Counters
- Plasma Surface Treatment Equipment
- Presses and Pellet Dies
- Surface Plasmon Resonance Instruments
- Ultrasonic Cleaners
- UV Disinfection Systems
- VOC Analysis Equipment
- VPHP Sterilization Systems
- Water Baths
- Lab Equipment
- Diagnostics & Clinical
- Applied Science
- Life Science
- Services
- About Us
- Contact Us
.
