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

Efipladib 是一种有效的、选择性的、具有口服活性的 cPLA2α 抑制剂，其 IC50 为 0.04 μM, Kd 为 0.067 μM。

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Efipladib Chemical Structure

Efipladib Chemical Structure

CAS No. : 381683-94-9

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Efipladib 相关抗体

Top Publications Citing Use of Products

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Phospholipase A PLD Phospholipase C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Efipladib is a potent, selective and orally active cPLA2α inhibitor with an IC50 of 0.04 μM and a Kd of 0.067 μM[1].

IC50 & Target[1]

cPLA2α

0.04 μM (IC50)

cPLA2α

0.067 μM (Ki)

体外研究
(In Vitro)

Efipladib (10-25 μM; 24-72 h) 增加 PC3 和 LNCaP 细胞中 COX-1 和 PGE2 水平[3]。

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

Efipladib 相关抗体:

Western Blot Analysis[3]

Cell Line: PC3 and LNCaP cells
Concentration: 10, 15, 20 and 25 μM
Incubation Time: 72 h
Result: Significantly decreased cPLA2α activity. Increased COX-1 protein levels. Increased COX-2 protein levels in PC3 cells.
体内研究
(In Vivo)

Efipladib (100 mg/kg; p.o.; BID for 31 days) 可逆转小鼠胶原性关节炎 (CIA) 模型的严重程度[1]。
Efipladib (100 mg/kg; p.o.; once) 在给药后 1 小时显著抑制大鼠完全弗氏佐剂 (CFA) 伤害感觉模型中的伤害反应[2]。
Efipladib 无法穿过血脑屏障进入中央室[2]。
Efipladib (100 nM; IT; 5 μL) 降低大鼠脑脊液 PGE2 水平[2]。

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

Animal Model: Mouse collagen-induced arthritis (CIA) model[1]
Dosage: 100 mg/kg
Administration: PO, BID for 31 days
Result: Gave a dramatic reduction in the clinical disease severity score relative to the vehicle treated group.
Animal Model: Male Sprague-Dawley rats[2]
Dosage: 100 nM in 5 μL of 100% DMSO/rat
Administration: Intrathecal administration
Result: Reduced PGE2 levels in the cerebrospinal fluid (CSF) by 45-60%, yet there was no effect on the nociceptive response.
分子量

746.14

Formula

C40H35Cl3N2O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Efipladib 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

Efipladib381683-94-9PhospholipaseCOX-1PGE2LNCaPPC3CFAarthritisInhibitorinhibitorinhibit

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目录号：
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