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.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description
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)
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
