Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ecopladib (PLA 725) 是一种胞浆磷脂酶 A2α (phospholipase A2α) 抑制剂,在 GLU micelle 和大鼠全血细胞中,IC50 值分别为 0.15 μM 和 0.11 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 13,900 | 现货 | ||
5 mg | ¥ 27,800 | 现货 | ||
10 mg | ¥ 37,800 | 现货 | ||
25 mg | ¥ 56,200 | 现货 | ||
50 mg | ¥ 75,900 | 现货 | ||
100 mg | ¥ 98,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 36,200 | 现货 |
产品描述 | 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. |
靶点活性 | cPLA2α, in GLU micelle:0.15 μM , cPLA2α, rat blood:0.11 μM |
体外活性 | 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.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[1]. |
体内活性 | 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]. |
别名 | 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)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.3367 mL | 6.6835 mL | 13.367 mL | 33.4175 mL |
5 mM | 0.2673 mL | 1.3367 mL | 2.6734 mL | 6.6835 mL | |
10 mM | 0.1337 mL | 0.6684 mL | 1.3367 mL | 3.3418 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ecopladib 381683-92-7 Metabolism Phospholipase PLA-725 PLA725 PLA 725 Inhibitor inhibitor inhibit