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Naproxen

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Chemical Structure| 22204-53-1 同义名 : (S)-Naproxen;(+)-Naproxen;Napratec;Naposin;CG 3117
CAS号 : 22204-53-1
货号 : A296148
分子式 : C14H14O3
纯度 : 98%
分子量 : 230.259
MDL号 : MFCD00010500
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(456.01 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 75 mg/mL(325.72 mM)
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 56 mg/mL suspension

生物活性
靶点

  • COX-2

    COX-2, IC50:5.2 μM

  • COX-1

    COX-1, IC50:8.7 μM
描述 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[3]. Both JNJ7777120 and naproxen exert an anti-inflammatory and antifibrotic effect that is increased by their combination, which could be an effective therapeutic strategy in the treatment of pulmonary fibrosis[4]. The IC(50) values (95% CI) of naproxen for analgesia (27 (0-130) μM), antipyretics (40 (30-65) μM) and inhibition of PGE(2) (13 (6-45) μM) were in similar range, whereas inhibition of TXB(2) (5 (4-8) μM) was observed at lower concentrations. Variability in the behavioral measurement of analgesia was larger than for the other endpoints[3]. Moreover, success rate on the treatment of neoplastic fever using naproxen was 94.1% (95% CI: 87.6%-97.3%). The success rate of the suspected neoplastic fever was 79.8%; for fever of unknown origin, it also reached 67.7%. Besides, a small dose of 125 mg naproxen, 375 mg twice a day and 250 mg 3 times a day were also useful[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01450995 Migraine Phase 4 Completed - United States, Tennessee ... 展开 >> Wesley Headache Clinic Memphis, Tennessee, United States, 38018 收起 <<
NCT00751400 - Completed - -
NCT01229228 Dental Pain Phase 2 Completed - United States, Texas ... 展开 >> Premier Research Group Limited Austin, Texas, United States, 78705 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.34mL

0.87mL

0.43mL

21.71mL

4.34mL

2.17mL

43.43mL

8.69mL

4.34mL
参考文献

[1]Krekels EH, Angesjo M, 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. Pharm Res. 2011 Jul;28(7):1561-76.

[2]Mitchell JA, Akarasereenont P, 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.

[3]Mitchell JA, Akarasereenont P, Thiemermann C, Flower RJ, Vane JR. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci U S A. 1993;90(24):11693-11697

[4]Rosa AC, Pini A, Lucarini L, et al. Prevention of bleomycin-induced lung inflammation and fibrosis in mice by naproxen and JNJ7777120 treatment. J Pharmacol Exp Ther. 2014;351(2):308-316

[5]Zhang H, Wu Y, Lin Z, et al. Naproxen for the treatment of neoplastic fever: A PRISMA-compliant systematic review and meta-analysis. Medicine (Baltimore). 2019;98(22):e15840