产品说明书

Oxaprozin

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Chemical Structure| 21256-18-8 同义名 : Oxaprozinum;Wy21743;Oxaprozin, Oxaprozinum, DL-8280, DR-3355, Hoe-280, ORF-28489, Ru-43280, Tarivid;NSC 310839
CAS号 : 21256-18-8
货号 : A395168
分子式 : C18H15NO3
纯度 : 99%
分子量 : 293.317
MDL号 : MFCD00215977
存储条件：

粉末 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(357.97 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
动物实验配方：
生物活性
靶点

  • COX-1
描述 Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin reversed in a dose-dependent manner immune complex-induced survival of monocytes, without affecting the apoptosis of resting cells. Other NSAIDs (Non-steroidal anti-inflammatory drugs) are ineffective. Oxaprozin-mediated inhibition of the Akt/IKK/NF-kappaB pathway contributes to its anti-inflammatory properties[3]. Among different NSAIDs, only oxaprozin dose-dependently increased apoptosis of CD40L-treated monocytes. Oxaprozin pro-apoptotic activity was associated with the inhibition of CD40L-triggered Akt and NF-kappaB phosphorylation and the activation of caspase 3[4].
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
NCT03350386 Healthy Phase 1 Completed - Japan ... 展开 >> P-One Clinic Hachiōji, Tokyo, Japan, 192-0071 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.41mL

0.68mL

0.34mL

17.05mL

3.41mL

1.70mL

34.09mL

6.82mL

3.41mL
参考文献

[1]Maestrelli F, Cirri M, et al. Improvement of oxaprozin solubility and permeability by the combined use of cyclodextrin, chitosan, and bile components. Eur J Pharm Biopharm. 2011 Aug;78(3):385-93.

[2]Kean WF. Oxaprozin: kinetic and dynamic profile in the treatment of pain. Curr Med Res Opin. 2004 Aug;20(8):1275-7.

[3]Ottonello L, Bertolotto M, Montecucco F, Bianchi G, Dallegri F. Delayed apoptosis of human monocytes exposed to immune complexes is reversed by oxaprozin: role of the Akt/IkappaB kinase/nuclear factor kappaB pathway. Br J Pharmacol. 2009;157(2):294-306

[4]Montecucco F, Bertolotto M, Ottonello L, Quercioli A, Mach F, Dallegri F. Oxaprozin-induced apoptosis on CD40 ligand-treated human primary monocytes is associated with the modulation of defined intracellular pathways. J Biomed Biotechnol. 2009;2009:478785