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编 号:F397427
分子式:C13H12Cl2O4
分子量:303.14
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10mM*1mL in DMSO
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50mg
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100mg
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生物活性:
Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma.

体内研究:
Ethacrynic acid (450 μg/mouse; 口服给药; 一天一次连续60天) 能够抑制小鼠中的胞瘤生长。Animal Model:Myeloma Balb/c mice model
Dosage:450 μg/mouse
Administration:Oral gavage (p.o.); Once daily for 60 days. After BALB/c mice were injected subcutaneously with 5 × 105 MPC11 myeloma cells.
Result:Significantly inhibited tumor growth.

体外研究:
Ethacrynic acid (50 μM; 24 小时) 抑制 CLL 细胞中 Wnt/β-catenin 的信号传导。Ethacrynic acid (1-100 μM; 48 小时) 在 CLL 细胞中具有细胞毒性,IC50 为 8.56 μM。Ethacrynic acid (0.01-0.25 mmol/L; 30 分钟) 增加眼睛的房水流出,出水率由28%提高到105%。Ethacrynic acid (10-100 μM; 30 分钟) 在 LPS (100 ng/mL) 诱导的 RAW264.7 细胞中能够抑制 NF-κB 通路的激活,具有抗炎活性。Ethacrynic acid (20 μM/mL; 2 小时) 可以增强经辐射照射后的 MCF-7 癌细胞中的辐射强度。Ethacrynic acid (100 μmol/L; 62.5-250分钟) 以剂量依赖性的方式抑制高 –K+ (80 mmol/L) 和乙酰胆碱 (acetylcholine, ACh, 100 μmol/L) 引起的小鼠气管环收缩,EC50 分别为 40.28 μmol/L 和 56.22 μmol/L。Ethacrynic acid (100 μmol/L; 500-2500 秒) 分别降低高 –K+ 和 ACh 诱导的细胞内 Ca2+ 浓度,分别从 0.40 降到 0.16,0.50 降到 0.39 。
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