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CAS No.: 80382-23-6

Loxoprofen sodium/洛索洛芬钠 Catalog No. CSN23658

Synonyms: Loxoprofen (sodium salt);Loxoprofen;洛索洛芬钠

Loxoprofen Sodium is a non-selective cyclooxygenase inhibitor, a nonsteroidal anti-inflammatory drug (NSAID) working by reducing the synthesis of prostaglandins from arachidonic acid.

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技术信息

生物活性

描述Loxoprofen sodium, an anti-inflammatory prodrug (NSAID), is a nonselective COX inhibitor with IC50s of 6.5 μM and 13.5 μM for COX-1 and COX-2 in human whole blood assays, respectively^[1]. Both loxoprofen sodium and celecoxib were well tolerated for the relief of acute postoperative pain after spinal surgery. A single administration of loxoprofen showed superior and rapid effectiveness compared with celecoxib for both slight and severe postoperative pain^[2]. In a rat air pouch model, oral administration of loxoprofen sodium lowered prostaglandin (PG) E2 in both fluid exudates of the inflammatory pouch and stomach tissue with ED50 values of 2.0 and 2.1 mg/kg, respectively. Additionally, platelet thromboxane B2 production was also inhibited by loxoprofen sodium (ED50 of 0.34 mg/kg). In a rat carrageenan-induced paw edema model, loxoprofen sodium dose-dependently reduced the paw edema, accompanied by a decrease in PGE2 content in inflamed paw exudates^[3].
参考文献

[1] Riendeau D, Salem M, Styhler A, Ouellet M, Mancini JA, Li CS. Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1201-3
[2] Sekiguchi H, Inoue G, Nakazawa T, Imura T, Saito W, Uchida K, Miyagi M, Takahira N, Takaso M. Loxoprofen sodium and celecoxib for postoperative pain in patients after spinal surgery: a randomized comparative study. J Orthop Sci. 2015 Jul;20(4):617-23
[3] Noguchi M, Kimoto A, Gierse JK, Walker MC, Zweifel BS, Nozaki K, Sasamata M. Enzymologic and pharmacologic profile of loxoprofen sodium and its metabolites. Biol Pharm Bull. 2005 Nov;28(11):2075-9

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
- 3.7274 mL
- 18.6372 mL
- 37.2745 mL
- 5 mM
- 0.7455 mL
- 3.7274 mL
- 7.4549 mL
- 10 mM
- 0.3727 mL
- 1.8637 mL
- 3.7274 mL

技术信息

CAS号

80382-23-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H17NaO3

运输

蓝冰

分子量

268.28

别名

Loxoprofen (sodium salt);Loxoprofen;洛索洛芬钠

溶解度

DMSO	Insoluble
Water	51.0 mg/mL (190.1 mM)
Ethanol	Insoluble

动物实验配方

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