Ecopladib
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 381683-92-7
- 分子式: C39H33Cl3N2O5S
- 分子量:748.11
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Phospholipase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
IC50: 0.15 μM (cPLA2α, in GLU micelle), 0.11 μM (cPLA2α, rat blood)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MC9 | IC50 |
20 nM
Compound: 123, ecopladib
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Inhibition of LTB4 production in mouse MC9 cells
Inhibition of LTB4 production in mouse MC9 cells
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[PMID: 17305324] |
| MC9 | IC50 |
20 nM
Compound: 123, ecopladib
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Inhibition of LTC4 production in mouse MC9 cells
Inhibition of LTC4 production in mouse MC9 cells
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[PMID: 17305324] |
| MC9 | IC50 |
20 nM
Compound: 123, ecopladib
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Inhibition of LTD4 production in mouse MC9 cells
Inhibition of LTD4 production in mouse MC9 cells
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[PMID: 17305324] |
| MC9 | IC50 |
20 nM
Compound: 123, ecopladib
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Inhibition of LTE4 production in mouse MC9 cells
Inhibition of LTE4 production in mouse MC9 cells
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[PMID: 17305324] |
| MC9 | IC50 |
20 nM
Compound: 123, ecopladib
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Inhibition of PGF2-alpha production in mouse MC9 cells
Inhibition of PGF2-alpha production in mouse MC9 cells
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[PMID: 17305324] |
体外実験
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 381683-92-7
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性状 Solid
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分子量 748.11
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分子式 C39H33Cl3N2O5S
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(OCCC2=C(CCNS(=O)(CC3=CC=C(Cl)C(Cl)=C3)=O)N(C(C4=CC=CC=C4)C5=CC=CC=C5)C6=C2C=C(Cl)C=C6)C=C1
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別名
PLA 725
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Ecopladib 関連分類
HY-U00037 関連分類
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