Triflusal

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Chemical Structure| 322-79-2 同义名 : 三氟醋柳酸 ;UR 1501
CAS号 : 322-79-2
货号 : A626746
分子式 : C10H7F3O4
纯度 : 97%
分子量 : 248.16
MDL号 : MFCD00866793
存储条件:

Pure form Sealed in dry, 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 Triflusal is a derivative of salicylic acid with a well-established platelet aggregation inhibitory profile. Triflusal is a potentially useful choice in the treatment and prophylaxis of brain ischemia[3]. Triflusal inhibited COX-2-mediated prostaglandin E2 (PGE2) production (IC50 = 0.16). Triflusal (but neither aspirin nor salicylate) produced a concentration-dependent inhibition of COX-2 protein expression in peripheral human mononuclear cells. In a rat air pouch model in vivo, in which both aspirin and triflusal inhibited PGE2 production (ID50 = 18.9 and 11.4 mg/kg p.o., respectively) but only triflusal-treated animals showed a decrease in COX-2 expression[4]. Triflusal (10 mg/kg i.v.) reduces platelet deposition on subendothelium-induced primary thrombus by about 68% in rabbits. Triflusal (10 mg/kg i.v.) reduces platelet deposition on a fresh thrombus formed over tunica media by about 48% in rabbits. Triflusal (40 mg/kg p.o.) reduces platelet deposition on a primary thrombus triggered by subendothelium and tunica media by 53% in rabbits. Triflusal (40 mg/kg p.o.) significantly reduces COX-2 mRNA levels and protein levels without influence COX-1 mRNA levels on the vascular wall in rabbits[5]. Triflusal (600 mg/day for 5 days) results in an increase in NO production by neutrophils and an increase in endothelial nitric oxide synthase (eNOS) protein expression in neutrophils in healthy volunteers[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.03mL

0.81mL

0.40mL

20.15mL

4.03mL

2.01mL

40.30mL

8.06mL

4.03mL

参考文献

[1]Duran X, Sanchez S, et al. Protective effects of triflusal on secondary thrombus growth and vascular cyclooxygenase-2. J Thromb Haemost. 2008 Aug;6(8):1385-92.

[2]Gonzalez-Correa JA, Arrebola MM, et al. Protective effect of triflusal and its main metabolite HTB in an in vitro model of anoxia-reoxygenation in rat brain slices: comparison with acetylsalicylic and salicylic acids. Naunyn Schmiedebergs Arch Pharmacol. 2005 Jan;371(1):81-8.

[3]González-Correa JA, De La Cruz JP. Triflusal: an antiplatelet drug with a neuroprotective effect? Cardiovasc Drug Rev. 2006 Spring;24(1):11-24

[4]Fernández de Arriba A, Cavalcanti F, Miralles A, Bayón Y, Alonso A, Merlos M, García-Rafanell J, Forn J. Inhibition of cyclooxygenase-2 expression by 4-trifluoromethyl derivatives of salicylate, triflusal, and its deacetylated metabolite, 2-hydroxy-4-trifluoromethylbenzoic acid. Mol Pharmacol. 1999 Apr;55(4):753-60

[5]X, Sánchez S, Vilahur G, Badimon L. Protective effects of triflusal on secondary thrombus growth and vascular cyclooxygenase-2. J Thromb Haemost. 2008 Aug;6(8):1385-92

[6]De Miguel LS, Jiménez A, Montón M, Farré J, Del Mar Arriero M, Rodríguez-Feo JA, García-Cañete J, Rico L, Gómez J, Núñez A, Casado S, Farré AL. A 4-trifluoromethyl derivative of salicylate, triflusal, stimulates nitric oxide production by human neutrophils: role in platelet function. Eur J Clin Invest. 2000 Sep;30(9):811-7