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 Vitro 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 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 Vivo Ecopladib 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:Solid IC50& Target:IC50: 0.15 μM (cPLA2α, in GLU micelle), 0.11 μM (cPLA2α, rat blood)
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Ecopladib
CAS number：381683-92-7 molecular formula：C39H33Cl3N2O5S
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| Chinese alias | 艾可拉迪 | ||
| English alias | Ecopladib | BDBM50205515 | PLA-725 | ECOPLADIB [INN] | DTXSID70191555 | Benzoic acid, 4-(2-(5-chloro-2-(2-((((3,4-dichlorophenyl)methyl)sulfonyl)amino)ethyl)-1-(diphenylmethyl)-1H-indol-3-yl)ethoxy) | Benzoic acid, 4-(2-(5-chloro-2-(2-((((3,4-dichlorophen | ||
| CAS number | 381683-92-7 | molecular formula | C39H33Cl3N2O5S |
| molecular weight | 748.11 g/mol | Exact mass | ≥95% |
| PSA | 106.000 Ų | logp | 9.500 |
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