Arachidonoyl thio-PC
(Synonyms: 2-deoxy-2-thio Arachidonoyl PC) 目录号 : GC42843
A PLA2 substrate
Cas No.:146797-82-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Arachidonoyl Thio-PC is a substrate for many phospholipase A2s (PLA2s) including sPLA2, cPLA2, and iPLA2. Cleavage of the sn-2 fatty acid by PLA2 results in generation of a free thiol which reacts with chromogenic reagents such as DTNB (Ellman's reagent) and DTP to allow quantitation of PLA2 activity. Isozyme-specific cPLA2 activity can be measured by excluding or inhibiting sPLA2 and iPLA2 activities in the assay.
| Cas No. | 146797-82-2 | SDF | |
| 别名 | 2-deoxy-2-thio Arachidonoyl PC | ||
| Canonical SMILES | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(S[C@@H](COP([O-])(OCC[N+](C)(C)C)=O)COCCCCCCCCCCCCCCCC)=O | ||
| 分子式 | C44H82NO6PS | 分子量 | 784.2 |
| 溶解度 | DMF: >25 mg/ml,DMSO: >25 mg/ml,Water: 0.5 mg/ml (per Suseela) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2752 mL | 6.3759 mL | 12.7518 mL |
| 5 mM | 0.255 mL | 1.2752 mL | 2.5504 mL |
| 10 mM | 0.1275 mL | 0.6376 mL | 1.2752 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Cytosolic phospholipase A2 regulation in the hibernating thirteen-lined ground squirrel
Cell Mol Biol Lett 2007;12(4):621-32.PMID:17728982DOI:10.2478/s11658-007-0036-8.
Cytosolic calcium-dependent phospholipase A(2) (cPLA(2)) has multiple roles including production of arachidonic acid (a key player in cellular signaling pathways) and membrane remodeling. Additionally, since catabolism of arachidonic acid generates free radicals, the enzyme is also implicated in ischemic injury to mammalian organs. Regulation of cPLA(2) could be important in the suppression and prioritization of cellular pathways in animals that undergo reversible transitions into hypometabolic states. The present study examines the responses and regulation of cPLA(2) in skeletal muscle and liver of hibernating thirteen-lined ground squirrels, Spermophilus tridecemlineatus. cPLA(2) activity decreased significantly by 43% in liver during hibernation, compared with euthermic controls, and K(m) values for Arachidonoyl thio-PC substrate fell in both organs during hibernation to 61% in liver and 28% in muscle of the corresponding euthermic value. To determine whether these responses were due to a change in the phosphorylation state of the enzyme, Western blotting was employed using antibodies recognizing phospho-Ser(505) on alpha-cPLA(2). The amount of phosphorylated alpha-cPLA(2) in hibernator liver was just 38% of the value in euthermic liver. Furthermore, incubation of liver extracts under conditions that enhanced protein phosphatase action caused a greater reduction in the detectable amount of phospho-Ser(505) enzyme content in euthermic, versus hibernator, extracts. The data are consistent with a suppression of cPLA(2) function during torpor via enzyme dephosphorylation, an action that may contribute to the well-developed ischemia tolerance and lack of oxidative damage found in hibernating species over cycles of torpor and arousal.
Effects of the inhibition of cytosolic phospholipase A(2)α in non-small cell lung cancer cells
J Cancer Res Clin Oncol 2012 May;138(5):827-35.PMID:22274867DOI:10.1007/s00432-012-1157-7.
Purpose: The aim of this study was to investigate the expression of cPLA(2)α in non-small lung cancer cell lines and tissues, and we sought to determine the in vitro effects of the pyrrolidine-2 inhibitor on cPLA(2)α sensitivity in three different non-small lung cancer cell lines. Methods: The expression of cPLA(2)α was determined in lung cancer cells by Western blot. Cytotoxicity, cell growth and inhibition of cPLA(2)α activity were determined in relation to the concentration of pyrrolidine-2. Finally, this study investigated immunohistochemical expressions of cPLA(2)α in 23 species of human non-small lung cancer and 5 species of human normal lung to assess their clinicopathological relevance. Results: cPLA(2)α is expressed in A549 and H460, however, no expression in H661 cells. Pyrrolidine-2 demonstrated a dose-dependent inhibitory effect on cell growth and its significantly inhibited BrdU incorporation of human non-small lung cancer cells. Inhibition with pyrrolidine-2 results in reduction in cPLA(2)α activity in A549 and H460 lung cancer cells by 50% when present at IC(50) concentration in Arachidonoyl thio-PC assay. Immunohistochemistry of human lung tissue revealed that cPLA(2)α is increased in lung cancer tissues. Conclusions: Pyrrolidine-2 is a more potent and specific cPLA(2)α inhibitor than MAFP and AACOCF3 and represents an excellent pharmacological tool to investigate the biosynthesis and the biological roles of cancer. The present study suggests that pyrrolidine-2 could be a potential therapeutic agent for cancer therapy.