Naproxen etemesil (Synonyms: LT-NS 001; MX 1094)
目录号: PL04920 纯度: ≥99%
CAS No. :385800-16-8
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中文名称
Naproxen etemesil
中文别名
2-methylsulfonylethyl (2S)-2-(6-methoxynaphthalen-2-yl)propanoate
英文名称
Naproxen etemesil
英文别名
NAPROXEN ETEMESIL;Naproxen etemesil [USAN];214269U36R;Naproxen etemesil (USAN);2-(methylsulfonyl)ethyl (S)-2-(6-methoxynaphthalen-2-yl)propanoate;DB12398;D10017;Q27253519;2-methylsulfonylethyl (2S)-2-(6-methoxynaphthalen-2-yl)propanoate;2-(Methylsulfonyl)ethyl (2S)-2-(6-methoxynaphthalen-2-yl)propanoate;2-Naphthaleneacetic acid, 6-methoxy-alpha-methyl-, 2-(methylsulfonyl)ethyl es;LT-NS 001;MX 1094
Cas No.
385800-16-8
分子式
C17H20O5S
分子量
336.40
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Naproxen etemesil 是一种亲脂性,非酸性,无活性的前体药物,一旦被吸收,Naproxen etemesil 就会水解成具有药理活性的Naproxen。Naproxen是COX-1 和 COX-2 的抑制剂,在细胞试验中 IC50 值分别为8.72 和5.15 μM。
生物活性
Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC 50 s of 8.72 and 5.15 μM, respectively in cell assay.
性状
Solid
IC50 & Target[1][2]
IC50: 8.72 μM (COX-1), 5.15 μM (COX-2)
体外研究(In Vitro)
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 IC50s of 2.2 μg/mL and 1.3 μg/mL, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Mitchell JA, et al. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci U S A. 1993 Dec 15;90(24):11693-7.
[2]. Rosa AC, et al. Prevention of bleomycin-induced lung inflammation and fibrosis in mice by naproxen and JNJ7777120 treatment. J Pharmacol Exp Ther. 2014 Nov;351(2):308-16.
溶解度数据
In Vitro: DMSO : 100 mg/mL (297.27 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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