AACOCF3 (Synonyms: ATK, AATFMK) |
Catalog No.GC16115 |
Inhibitor of cPLA2/anandamide hydrolysis/FAAH
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 149301-79-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
Cas No. | 149301-79-1 | SDF | |
Synonyms | ATK, AATFMK | ||
Chemical Name | 1,1,1-trifluoro-6Z,9Z,12Z,15Z-heneicosatetraen-2-one | ||
Canonical SMILES | FC(F)(C(CCC/C=C\C/C=C\C/C=C\C/C=C\CCCCC)=O)F | ||
Formula | C21H31F3O | M.Wt | 356.47 |
Solubility | DMF: >25 mg/ml,DMSO: > 25 mg/ml,PBS pH 7.2: <50 µ g/ml | Storage | Store at -20°C, protect from light |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.8053 mL | 14.0264 mL | 28.0529 mL |
5 mM | 0.5611 mL | 2.8053 mL | 5.6106 mL |
10 mM | 0.2805 mL | 1.4026 mL | 2.8053 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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