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Thioetheramide-PC
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Thioetheramide-PC图片
CAS NO:116457-99-9
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Cas No.116457-99-9
别名1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
化学名1,2-dideoxy-1-(S-hexadecyl)thio-2-(N-hexadecanoyl)amino-sn-glyceryl-3-phosphorylcholine
Canonical SMILESCCCCCCCCCCCCCCCC(N[C@@H](COP(OCC[N+](C)(C)C)([O-])=O)CSCCCCCCCCCCCCCCCC)=O
分子式C40H83N2O5PS
分子量735.1
溶解度4.25 mM Triton X-100: soluble (per reference),Ethanol: 10 mg/ml (@ roomtemp)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Thioetheramide-PC is a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2) [1]. Thioetheramide-PC is a structurally modified phospholipid.

PLA2s hydrolyze the sn-2 ester bond of phospholipids, releasing fatty acids and lysophospholipids, both of which may alter cell function. PLA2s play vital roles in cellular signaling and a wide number of pathophysiological situations, ranging from systemic and acute inflammatory conditions to cancer [2]. sPLA2 promote inflammation in mammals. High levels of sPLA2 contributes to several inflammatory diseases, and has been shown to promote vascular inflammation correlating with coronary events in coronary artery disease and acute coronary syndrome, and possibly leading to acute respiratory distress syndrome and progression of tonsillitis [3].

Thioetheramide-PC inhibited secretory phospholipase A2 (sPLA2) by binding to the catalytic site of sPLA2. The IC50 value was 2 μM [1]. Thioetheramide-PC could also bind to the activator site of this enzyme, which was tighter than its binding to the catalytic site. This dual interaction was that at low concentrations thioetheramide-PC might activate phospholipase activity rather than inhibiting it [1].

References:
[1] Yu L, Deems R A, Hajdu J, et al.  The interaction of phospholipase A2 with phospholipid analogues and inhibitors[J]. Journal of Biological Chemistry, 1990, 265(5): 2657-2664.
[2] Balsinde J, Balboa M A, Insel P A, et al.  Regulation and inhibition of phospholipase A2[J]. Annual Review of Pharmacology and Toxicology, 1999, 39(1): 175-189.
[3] Mallat Z, Lambeau G, Tedgui A.  Lipoprotein-associated and secreted phospholipases A2 in cardiovascular disease[J]. Circulation, 2010, 122(21): 2183-2200.