5.30538

cPLA2α Inhibitor II, Pyrrophenone

• 别名: cPLA2α Inhibitor II, Pyrrophenone, Phospholipase A2α Inhibitor
• 经验公式（希尔记法）: C₄₉H₃₇F₂N₃O₅S₂
• CAS号: 341973-06-6
• 分子量: 849.96
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: powder
• 效力: 4.2 nM IC₅₀
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: −20°C

说明

一般說明

Pyrrophenone is a cell-permeable, non-toxic, pyrolidine derivative that acts as a highly potent, and reversible inhibitor of cytosolic phospholipase A2a (cPLA2a; IC50 = 4.2 nM). Does not inhibit the activities of PLA IB and IIA groups even at higher concentrations (~250 µM). Unlike AACOCF3 (Cat. No. 100109), its action is shown to be rapid and does not require a pre-incubation period. Diminishes the release of arachidonic acid (IC50 = 24 nM), prostaglandin E2 (PGE2; IC50 = 25 nM) and leukotriene C4 (IC50 = 14 nM) in A23187 stimulated THP-1 cells. Its effects on production of PGE2 and thromboxane B2 are comparable to those of indomethacin. Also shown to inhibit the lysophospholipase and esterase activity of cPLA2&alpha.

生化／生理作用

Cell permeable: yes

Primary Target
PLA2a

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他說明

Please note that the molecular weight for this compound is batch-specific due to variable water content.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable