Thioetheramide-PC (Synonyms: 1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine) |
رقم الكتالوجGC11116
One-Click Copy Product Info
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competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 116457-99-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 116457-99-9 | SDF | |
| المرادفات | 1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine | ||
| Chemical Name | 1,2-dideoxy-1-(S-hexadecyl)thio-2-(N-hexadecanoyl)amino-sn-glyceryl-3-phosphorylcholine | ||
| Canonical SMILES | CCCCCCCCCCCCCCCC(N[C@@H](COP(OCC[N+](C)(C)C)([O-])=O)CSCCCCCCCCCCCCCCCC)=O | ||
| Formula | C40H83N2O5PS | M.Wt | 735.1 |
| الذوبان | 4.25 mM Triton X-100: soluble (per reference),Ethanol: 10 mg/ml (@ roomtemp) | Storage | Store at -20°C |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3604 mL | 6.8018 mL | 13.6036 mL |
| 5 mM | 272.1 μL | 1.3604 mL | 2.7207 mL |
| 10 mM | 136 μL | 680.2 μL | 1.3604 mL |
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Working concentration: mg/ml;
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)