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CAS No.: 21256-18-8

奥沙普秦 Catalog No. CSN12602

Synonyms: Oxaprozinum;Wy21743;NSC 310839

Oxaprozin is a COX inhibitor with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, it's a NSAID used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis.

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实验方案

技术信息

生物活性

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 ... more >> P-One Clinic Hachiōji, Tokyo, Japan, 192-0071 Collapse <<

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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4093 mL
- 17.0464 mL
- 34.0929 mL
- 5 mM
- 0.6819 mL
- 3.4093 mL
- 6.8186 mL
- 10 mM
- 0.3409 mL
- 1.7046 mL
- 3.4093 mL

技术信息

CAS号

21256-18-8

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H15NO3

运输

蓝冰

分子量

293.32

别名

Oxaprozinum;Wy21743;NSC 310839;DL-8280;DR-3355;Hoe-280;ORF-28489;Ru-43280;Tarivid;奥沙普秦

溶解度

DMSO	140.0 mg/mL (477.3 mM)
Water	insoluble

动物实验配方

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