| 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/Shipping at ambient temperature. |
| Solubility Information | DMSO : 7.49 mg/mL (10.01 mM), Sonication is recommended.
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| Keywords | PLA-725 | PLA725 | Ecopladib | cPLA2α, rat blood | cPLA2α, in GLU micelle | cPLA2α |
| Inhibitors Related | Neomycin sulfate | Levamisole hydrochloride | 1-Naphthaleneacetic acid potassium salt | Difluprednate | trans-Benzylideneacetone | Benzylideneacetone | Omeprazole | Indomethacin | Darapladib | 1-Naphthaleneacetic acid | Lansoprazole | Magnesium sulfate |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Inhibitor Library | Metabolism Compound Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max |
United States
