Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |
---|---|---|---|
1 mg | 在庫あり | ¥ 319,000 | |
5 mg | 在庫あり | ¥ 640,500 | |
10 mg | 在庫あり | ¥ 865,500 | |
25 mg | 在庫あり | お問い合わせ | |
50 mg | 在庫あり | お問い合わせ | |
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 824,000 |
説明 | 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. |
ターゲット&IC50 | CPLA2α (GLU micelle):0.15 μM , CPLA2α (rat blood):0.11 μM |
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]. |
別名 | PLA 725 |
分子量 | 748.11 |
分子式 | C39H33Cl3N2O5S |
CAS No. | 381683-92-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.48 mg/mL (10 mM)
You can also refer to dose conversion for different animals. 詳細
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Ecopladib 381683-92-7 Metabolism Phospholipase PLA-725 PLA725 PLA 725 Inhibitor inhibitor inhibit