385800-16-8
中文名稱
(S)-2-(甲磺酰)乙基 2-(6-甲氧基萘-2-基)丙酯
英文名稱
(S)-2-(methylsulfonyl)ethyl 2-(6-methoxynaphthalen-2-yl)propanoate(WXG02261)
CAS
385800-16-8
分子式
C17H20O5S
分子量
336.4
MOL 文件
385800-16-8.mol
385800-16-8 結構式
基本信息
中文別名
(S)-2-(甲磺酰)乙基 2-(6-甲氧基萘-2-基)丙酯 英文別名
MX 1094LT-NS 001
Naproxen etemesil
(S)-2-(methylsulfonyl)ethyl 2-(6-methoxynaphthalen-2-yl)propanoate
(S)-2-(methylsulfonyl)ethyl 2-(6-methoxynaphthalen-2-yl)propanoate(WXG02261)
2-Naphthaleneacetic acid, 6-methoxy-α-methyl-, 2-(methylsulfonyl)ethyl ester, (αS)-
物理化學性質
沸點542.0±35.0 °C(Predicted)
密度1.238±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
Naproxen etemesil 是一種親脂性，非酸性，無活性的前體藥物，一旦被吸收，Naproxen etemesil 就會水解成具有藥理活性的Naproxen。Naproxen是COX-1 和 COX-2 的抑制劑，在細胞試驗中 IC50 值分別為8.72 和5.15 μM。靶點
IC50: 8.72 μM (COX-1), 5.15 μM (COX-2)
體外研究
Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a well known nonsteroidal anti-inflammatory drug. Naproxen is approximately equipotent inhibitor of COX-1 and COX-2 in intact cells with IC 50 s of 2.2 μg/mL and 1.3 μg/mL, respectively.
體內研究
Naproxen exerts an anti-inflammatory and antifibrotic effect in mouse model of bleomycin-induced lung fibrosis. Naproxen also downregulates TGF-β levels and Smad3/4 complex formation. Naproxen is shown to inhibit the time-courses of pain, fever and PGE2 with similar potencies (IC 50 =27, 40, 13 μM).