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  2. Metabolic Enzyme/Protease
  3. Phospholipase
  4. Ecopladib

Ecopladib  (Synonyms: PLA 725)

目錄號(hào): HY-U00037 純度: 95.0%
COA 產(chǎn)品使用指南

Ecopladib 是一種胞漿磷脂酶 A2α (phospholipase A2α) 抑制劑，在 GLU micelle 和大鼠全血細(xì)胞中，IC50 值分別為 0.15 μM 和 0.11 μM。

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Ecopladib Chemical Structure

Ecopladib Chemical Structure

CAS No. : 381683-92-7

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1 mg ￥16800
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查看 Phospholipase 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.

IC50 & Target

IC50: 0.15 μM (cPLA2α, in GLU micelle), 0.11 μM (cPLA2α, rat blood)[1]
體外研究
(In Vitro)

Ecopladib inhibits cPLA2α in the PAPE liposome assay at 73% at a concentration of 37 nM, while it inhibits sPLA2 at 16% at 1 μM. Ecopladib inhibits the production of prostaglandins (PGF2α) and leukotrienes (LTB4 and LTC4/D4/E4) with comparable IC50s of 20?30 nM. Ecopladib is inactive against COX-1 and COX-2 at 20 μM, which is nearly 100 times the IC50 in the MC-9 cells. Ecopladib inhibit 12- and 15-HETE, which are derived from arachidonic acid via the 12- and 15-lipoxygenase pathways and the IC50s are ～0.3 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Ecopladib is orally efficacious in this model and displays an ED50 of 8 mg/kg, demonstrating that it can inhibit COX-2 derived PGE2 formation in vivo. Ecopladib is orally efficacious at reducing carrageenan-induced paw swelling:?from dose?response studies, it is determined that the ED50 is 40 mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

748.11

Formula

C39H33Cl3N2O5S
CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
純度 & 產(chǎn)品資料
參考文獻(xiàn)
Animal Administration
[1]

Male Sprague?Dawley rats are anesthetized, and 10?20 mL of filtered air is injected subcutaneously under the dorsal skin to form a pouch. Three and six days later, the pouches are reinflated with 10?15 mL of sterile air. On the seventh day, the test compound is dissolved in vehicle (55.5% Phosal 53 MCT, 5.6% Tween 80, 16.7% Labrasol, and 22.2% propylene carbonate) to give 37.5 mg of test compound per mL of vehicle. This test compound in vehicle is diluted with water to the appropriate concentration and dosed at 4 mL/kg. Vehicle treated animals receives the same amount of vehicle as the animals treated with the highest dose of compound. Two hours later, 2 mL of a 1% solution of carrageenan (Viscarin carrageenan type GP-209NF) in saline is injected into the pouch. Six hours after the carrageenan injection, the rats are individually sacrificed and the contents of the pouch are harvested. The amount of fluid recovered is measured. An aliquot of the exudate is centrifuged at 6500 rpm for 10 min, and 300 μL of each supernatant is precipitated with MeOH (800 μL) precooled to 0°C. The samples are well vortexed and are kept at ?80°C overnight. The samples are centrifuged again and assayed for PGE2 to locate the PGE2 production within the linear range of the PGE2 standard curve. To minimize the difference in binding environments for the standards and samples, the standard curve is generated in a 1% solution of carrageenan that is mixed with assay buffer to the same dilution as the samples. The approximate ED50 value is extrapolated from the dose?response curve.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱(chēng)：
Ecopladib
目錄號(hào)：
HY-U00037
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