Ecopladib 是一种胞浆磷脂酶 A2α (Phospholipase A2α) 抑制剂，在 GLU micelle 和大鼠全血细胞中，IC50 值分别为 0.15 μM 和 0.11 μM。

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.

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.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[1].

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].

381683-92-7

C39H33Cl3N2O5S

748.11

PLA 725

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years