| Name | Ecopladib |
| Description | Ecopladib (PLA 725) 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. |
| In vitro | Ecopladib is inactive against COX-1 and COX-2 at a concentration of 20 μM, significantly higher than its IC50 in MC-9 cells. It effectively inhibits 12- and 15-HETE production through the 12- and 15-lipoxygenase pathways, with IC50 values around 0.3 μM. Furthermore, Ecopladib shows a 73% inhibition of cPLA2α at 37 nM in the PAPE liposome assay and a 16% inhibition of sPLA2 at 1 μM. It also suppresses the generation of prostaglandins (PGF2α) and leukotrienes (LTB4 and LTC4/D4/E4), with IC50 values ranging between 20−30 nM, demonstrating its effectiveness across multiple pathways involved in inflammation and cell signaling. |
| 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.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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 7.48 mg/mL (10 mM)
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| Keywords | PLA-725 | PLA725 | Ecopladib |
| Inhibitors Related | Neomycin sulfate | 1-Naphthaleneacetic acid potassium salt | trans-Benzylideneacetone | Benzylideneacetone | Tris(2,4-di-tert-butylphenyl)phosphate | (E/Z)-Polydatin | Indomethacin | Fluticasone (propionate) | 1-Naphthaleneacetic acid | Darapladib | Lansoprazole | Amentoflavone |
| Related Compound Libraries | Bioactive Compound Library | Inhibitor Library | Bioactive Compounds Library Max |
United States
