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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 475 € | In Stock | |
5 mg | 950 € | In Stock | |
10 mg | 1.282 € | In Stock | |
25 mg | 1.871 € | In Stock | |
50 mg | 2.555 € | In Stock | |
100 mg | 3.477 € | In Stock |
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 (rat blood):0.11 μM , CPLA2α (GLU micelle):0.15 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]. |
Alias | PLA 725 |
Molecular Weight | 748.11 |
Formula | C39H33Cl3N2O5S |
Cas No. | 381683-92-7 |
Smiles | OC(=O)c1ccc(OCCc2c(CCNS(=O)(=O)Cc3ccc(Cl)c(Cl)c3)n(C(c3ccccc3)c3ccccc3)c3ccc(Cl)cc23)cc1 |
Relative Density. | 1.35g/cm3 |
Storage | Powder: -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
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