Loxoprofen sodium

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Chemical Structure| 80382-23-6 同义名 : Loxoprofen (sodium salt)
CAS号 : 80382-23-6
货号 : A100810
分子式 : C15H17NaO3
纯度 : 97%
分子量 : 268.28
MDL号 : MFCD00941425
存储条件:

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.73mL

0.75mL

0.37mL

18.64mL

3.73mL

1.86mL

37.27mL

7.45mL

3.73mL

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