产品
编 号：F342525
分子式：C39H33Cl3N2O5S
分子量：748.11
分子式：C39H33Cl3N2O5S
分子量：748.11
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 381683-92-7
产品详情
生物活性：
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.
体内研究：
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. Ecopladib is orally efficacious at reducing carrageenan-induced paw swelling:?from dose?response studies, it is determined that the ED50 is 40 mg/kg.
体外研究：
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. 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 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.
体内研究：
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. Ecopladib is orally efficacious at reducing carrageenan-induced paw swelling:?from dose?response studies, it is determined that the ED50 is 40 mg/kg.
体外研究：
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. 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.
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