Thioetheramide-PC

Thioetheramide-PC

Catalog Number:
L002373118APE
Mfr. No.:
APE-C4894
Price:
$289
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine; 1,2-dideoxy-1-(S-hexadecyl)thio-2-(N-hexadecanoyl)amino-sn-glyceryl-3-phosphorylcholine
          CAS Number
          116457-99-9
          Molecular Formula
          C40H83N2O5PS
          Molecular Weight
          735.1
          Appearance
          A solution in ethanol. To change the solvent, simply evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
          Purity
          Purity ≥ 95.00%
          Solubility
          Soluble in DMSO;Soluble in dimethyl formamide
          Storage
          Store at -20°C

          * For Research Use Only

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