PACOCF3

Antagonizes DP receptor agonist effects

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
1mg

￥200.00

160.00

- +
5mg

￥562.00

450.00

- +
10mg

￥775.00

620.00

- +
25mg

￥1450.00

1160.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajci17670
CAS: 141022-99-3
别名: 1,1,1-三氟-2-十七烷酮,Palmityltrifluoromet?hylketone
分子式: C17H31F3O
分子量: 308.43
纯度: >98%
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: Desiccate at -20°C
库存: 现货

Background

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.

参考文献:
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.