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Ecopladib

Catalog No. T11149Cas No. 381683-92-7
Alias PLA 725

Ecopladib (PLA 725) 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.

Ecopladib

Ecopladib

Purity: 99.02%
Catalog No. T11149Alias PLA 725Cas No. 381683-92-7
Ecopladib (PLA 725) 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.
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1 mg$834In Stock
5 mg$1,670In Stock
10 mg$2,260In Stock
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Purity:99.02%
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Product Introduction

Bioactivity
Description
Ecopladib (PLA 725) 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.
Targets&IC50
CPLA2α (GLU micelle):0.15 μM , CPLA2α (rat blood):0.11 μM
In vitro
Ecopladib is inactive against COX-1 and COX-2 at a concentration of 20 μM, significantly higher than its IC50 in MC-9 cells. It effectively inhibits 12- and 15-HETE production through the 12- and 15-lipoxygenase pathways, with IC50 values around 0.3 μM. Furthermore, Ecopladib shows a 73% inhibition of cPLA2α at 37 nM in the PAPE liposome assay and a 16% inhibition of sPLA2 at 1 μM. It also suppresses the generation of prostaglandins (PGF2α) and leukotrienes (LTB4 and LTC4/D4/E4), with IC50 values ranging between 20−30 nM, demonstrating its effectiveness across multiple pathways involved in inflammation and cell signaling.
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.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[1].
AliasPLA 725
Chemical Properties
Molecular Weight748.11
FormulaC39H33Cl3N2O5S
Cas No.381683-92-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 7.48 mg/mL (10 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.3367 mL6.6835 mL13.3670 mL66.8351 mL
5 mM0.2673 mL1.3367 mL2.6734 mL13.3670 mL
10 mM0.1337 mL0.6684 mL1.3367 mL6.6835 mL

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