Ecopladib

Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α) , with IC 50 s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.In VitroEcopladib 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 IC 50 s of 20−30 nM. Ecopladib is inactive against COX-1 and COX-2 at 20 μM, which is nearly 100 times the IC 50 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 IC 50 s are ∼0.3 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoEcopladib is orally efficacious in this model and displays an ED 50 of 8 mg/kg, demonstrating that it can inhibit COX-2 derived PGE2 formation in vivo. Ecopladib is orally efficacious at reducing carrageenan-induced paw swelling: from dose−response studies, it is determined that the ED 50 is 40 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 0.15 μM (cPLA2α, in GLU micelle), 0.11 μM (cPLA2α, rat blood). Specification: 0.95 Molecular Formula: C39H33Cl3N2O5S Molecular Weight: 748.11 PubChem CID: 204106 Isomeric SMILES: C1=CC=C(C=C1)C(C2=CC=CC=C2)N3C4=C(C=C(C=C4)Cl)C(=C3CCNS(=O)(=O)CC5=CC(=C(C=C5)Cl)Cl)CCOC6=CC=C(C=C6)C(=O)O