PACOCF3 (Palmityltrifluoromethylketone) 是一种选择性磷脂酶 A2 抑制剂，IC50 为 3.8 μM。
| Cas No. | 141022-99-3 |
| 别名 | 1,1,1-三氟-2-十七烷酮,Palmityltrifluoromet?hylketone |
| 化学名 | 1,1,1-trifluoroheptadecan-2-one |
| Canonical SMILES | FC(F)(C(CCCCCCCCCCCCCCC)=O)F |
| 分子式 | C17H31F3O |
| 分子量 | 308.43 |
| 溶解度 | basic PBS: freely soluble,DMF: >50 mg/ml,DMSO: >30 mg/ml,Ethanol: >50 mg/ml,PBS pH 7.2:<50 µ g/ml (from ATK) |
| 储存条件 | Desiccate at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | PACOCF3 is a inhibitor of both Ca2+-dependent cytosolic cPLA2 and Ca2+-independent phospholipases A2 iPLA2 with IC50 values of 45 μM and 3.8 μM [1,2], which is an innovate and potential candidate drug for inflammation, atherosclerosis, diabetes mellitus, therapeutic shock, cancer therapyetc [3,4,5,6]. It has been reported that PACOCF3 can inhibit PLA2 and reduce the inflammatory response. PACOCF3 also can stimulate insulin release at basal glucose levels (2 mmol/l). Application of PACOCF3 can inhibit endogenous arachidonic acid generation which significantly decreased the amplitude of the insulin secretory response to 20 mmol/l glucose [7,8]. PACOCF3 have a dual protective role in diabetes which could minimize β-cell dysfunction while maintaining insulin secretory output through enhancing endogenous arachidonic acid levels. References:
1. Murakami M et al.Emerging roles of secreted phospholipase A2 enzymes: The 3rd edition.Biochimie. 2014 Sep 16. pii: S0300-9084(14)00252-1.
2. Quach ND et al. Secretory phospholipase A2 enzymes as pharmacological targets for treatment of disease. Biochem Pharmacol. 2014 Aug 15;90(4):338-48.
3. Chalimoniuk M. Secretory phospholipase A2 and its role in oxidative stress and inflammation]. Postepy Biochem. 2012;58(2):204-8.
4. Persaud SJ.et al. The role of arachidonic acid and its metabolites in insulin secretion from human islets of langerhans. Diabetes. 2007 Jan;56(1):197-203.
5. Khakpour H et al. Lipoprotein-associated phospholipase A2: an independent predictor of cardiovascular risk and a novel target for immunomodulation therapy. Cardiol Rev. 2009 Sep-Oct;17(5):222-9.
6. Narendra Sharath Chandra JN1 et al. Chemistry and structural evaluation of different phospholipase A2 inhibitors in arachidonic acid pathway mediated inflammation and snake venom toxicity. Curr Top Med Chem. 2007;7(8):787-800.
7. Packard CJ. Lipoprotein-associated phospholipase A2 as a biomarker of coronary heart disease and a therapeutic target. Curr Opin Cardiol. 2009 Jul;24(4):358-63.
8. Lucas R et al. Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2. Bioorg Med Chem Lett. 2000 Feb 7;10(3):285-8. |
