| CAS |
No.22204-53-1 |
| 中文名称 |
萘普生(10mM in DMSO,无菌） |
| 英文名称 |
Naproxen(10mM in DMSO，Sterile） |
| 分子式 |
C14H14O3 |
| 分子量 |
230.26 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
COX |
| 通路 |
Immunology & Inflammation |
| 背景说明 |
Naproxen是COX-1 和 COX-2 的抑制剂。 |
| 生物活性 |
Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM， respectively in cell assay.[1-3] |
| In Vitro |
Naproxen etemesil 是一种亲脂性、非酸性、无活性的 Naproxen 前药，一旦被吸收就会水解成具有药理活性的 Naproxen。Naproxen 是众所周知的非甾体抗炎药。Naproxen 在完整细胞中是近似等效的 COX-1 和 COX-2 抑制剂，IC50 分别为 2.2 μg/mL 和 1.3 μg/mL[1]。 |
| In Vivo |
Naproxen 在博来霉素诱导的肺纤维化小鼠模型中发挥抗炎和抗纤维化作用。Naproxen 还下调 TGF-β 水平和 Smad3/4 复合物形成[2]。Naproxen 显示出抑制疼痛、发热和 PGE2 的时间过程，具有相似的效力 (IC50=27、40、13 μM)[3]。 |
| 细胞实验 |
BAEC are incubated for 30 min with Naproxen (0.1 ng/mL to 1 mg/mL). Arachidonic acid (30 μM) is then added， and the cells are incubated for a further 15 min at 37°C. The medium is then removed， and radioimmunoassay is used to measure the formation of 6-keto-PGF，a， PGE2， thromboxane B2， or PGF2a[1]. |
| 动物实验 |
Rats[3]To measure the analgesic effects of naproxen in a carrageenaninduced model of monoarthritis， Male Sprague–Dawley rats (n=48， 217±28 g) are randomly divided into four groups of 12 by an internally developed computer program， allowing the blind performance of the behavioral experiment. To induce hyperalgesia by inflammation， animals in groups 1B， 1C， and 1D receive a 40-μL intra-articular injection of a saline solution containing 7.5 mg/mL carrageenan in the left hind limb under isoflurane anesthesia (time=?1 h). Animals in group 1A receive no injection. After 1 h (time=0) the animals in groups 1A， 1B， 1C， and 1D receive oral doses of naproxen in saline of 0， 0， 7.5 and 30 μmol/kg， respectively. The doses and time points of measurements are selected on the basis of simulations predicting measuring a full concentration-effect relationship within the time-span of the experiment[3].Mice[2]Bleomycin (0.05 IU) is instilled intratracheally to C57BL/6 mice， which are then treated by micro-osmotic pump with vehicle， JNJ7777120 (40 mg/kg b.wt.)， naproxen (21 mg/kg b.wt.)， or a combination of both. Airway resistance to inflation， an index of lung stiffness， is assessed， and lung specimens are processed for inflammation， oxidative stress， and fibrosis markers[2]. |
| 数据来源文献 |
[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.
[3]. Krekels EH， et al. Pharmacokinetic-pharmacodynamic modeling of the inhibitory effects of naproxen on the time-courses of inflammatory pain， fever， and the ex vivo synthesis of TXB2 and PGE2 in rats. |
| 规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
| 单位 |
瓶 |
中文
英语
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