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Ecopladib

Catalog No. T11149   CAS 381683-92-7
Synonyms: 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.

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Ecopladib Chemical Structure
Ecopladib, CAS 381683-92-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 1,390.00
5 mg In stock $ 2,790.00
10 mg In stock $ 3,770.00
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1 mL * 10 mM (in DMSO) In stock $ 3,590.00
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Purity: 99.02%
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Biological Description
Chemical Properties
Storage & Solubility Information
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].
Synonyms PLA 725
Molecular Weight 748.11
Formula C39H33Cl3N2O5S
CAS No. 381683-92-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 7.48 mg/mL (10 mM)

TargetMolReferences and Literature

1. Lee KL, et al. Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha. J Med Chem. 2007 Mar 22;50(6):1380-400. Epub 2007 Feb 17.

Related compound libraries

This product is contained In the following compound libraries:
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Benzylideneacetone U-73343 Lp-PLA2-IN-1 ASM-IN-1 Lp-PLA2-IN-15 Vinaxanthone 1-Naphthaleneacetic acid potassium salt Carbazochrome

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Keywords

Ecopladib 381683-92-7 Metabolism Phospholipase PLA-725 PLA725 PLA 725 inhibitor inhibit

 

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