|2-乙酰氧基-4-(三氟甲基)苯甲酸|CsnPharm

CAS No.: 322-79-2

Triflusal/三氟柳 Catalog No. CSN16812

Synonyms: UR1501;Disgren;Grendis

Triflusal inhibits the production of thromboxane-B2 in platelets irreversibly by acetylating cycloxygenase-1.

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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].
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
NCT00162799	Insulin Resistance	Phase 2	Completed	-	Spain ... more >> Unitat de Diabetologia, Endocrinologia y Nutrición Hosp Josep Trueta Girona, Spain, 17007 Collapse <<
NCT03243409	-	-	Recruiting	August 31, 2017	Spain ... more >> Hospital de la Santa Creu i Sant Pau Recruiting Barcelona, Spain, 08025 Contact: Laura Noguera, MD lnoguera@santpau.cat Collapse <<
NCT01612273	Vasospastic Syndrome	Phase 4	Completed	-	Korea, Republic of ... more >> Division of Cardiology, Department of Internal Medicine, severance hospital Seoul, Korea, Republic of, 120-752 Collapse <<

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参考文献

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
- 4.0297 mL
- 20.1487 mL
- 40.2973 mL
- 5 mM
- 0.8059 mL
- 4.0297 mL
- 8.0595 mL
- 10 mM
- 0.4030 mL
- 2.0149 mL
- 4.0297 mL

技术信息

CAS号

322-79-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H7F3O4

运输

蓝冰

分子量

248.16

别名

UR1501;Disgren;Grendis;Aflen;Triflux;三氟柳

溶解度

DMSO	270.0 mg/mL (1088.0 mM)
Water	11.0 mg/mL (44.3 mM) warming

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00162799	Insulin Resistance	Phase 2	Completed	-	Spain ... more >> Unitat de Diabetologia, Endocrinologia y Nutrición Hosp Josep Trueta Girona, Spain, 17007 Collapse <<
NCT03243409	-	-	Recruiting	August 31, 2017	Spain ... more >> Hospital de la Santa Creu i Sant Pau Recruiting Barcelona, Spain, 08025 Contact: Laura Noguera, MD lnoguera@santpau.cat Collapse <<
NCT01612273	Vasospastic Syndrome	Phase 4	Completed	-	Korea, Republic of ... more >> Division of Cardiology, Department of Internal Medicine, severance hospital Seoul, Korea, Republic of, 120-752 Collapse <<
NCT02616497	Atherothrombosis	Phase 4	Completed	-	Greece ... more >> Atherothrombosis Research Centre / Laboratory of Biochemistry, University of Ioannina Ioannina, Greece, 45110 Collapse <<
NCT01174693	Cerebral Infarction	Phase 4	Completed	-	Korea, Republic of ... more >> Department of Neurology, Wonju Christian Hospital, Yonei University Wonju College of Medicine Wonju-si, Gangwon-do, Korea, Republic of, 220-701 Department of Neurology, National Health Insurance Corporation Ilsan Hospital Goyang-si, Gyeonggi-do, Korea, Republic of, 410-719 Department of Neurology, CHA Bundang Medical Center, CHA University School of Medicine Seongnam-si, Gyeonggi-do, Korea, Republic of, 463-712 Changwon Fatima Hospital Changwon, Gyeongsangnam-do, Korea, Republic of, 641-560 Keimyung University Dongsan Medical Center Daegu, Korea, Republic of, 700-712 Kyungpook National University Hospital Daegu, Korea, Republic of, 700-721 Yeungnam University Hospital Daegu, Korea, Republic of, 705-717 Department of Neurology, Konyang University Hospital Daejeon, Korea, Republic of, 302-718 Department of Neurology, Chosun University Hospital Gwangju, Korea, Republic of, 501-717 Department of Neurology, National Medical Center Seoul, Korea, Republic of, 100-799 Department of Neurology, Severance Hospital, Yonsei University College of Medicine Seoul, Korea, Republic of, 120-752 KyungHee University Medical Center Seoul, Korea, Republic of, 130-702 Department of Neurology, Kyung Hee University Hospital at Gangdong Seoul, Korea, Republic of, 134-727 Department of Neurology, Gangnam Severance Hospital, Yonsei Univ. College of Medicine Seoul, Korea, Republic of, 135-720 Korea University Anam Hospital Seoul, Korea, Republic of, 136-705 Department of Neurology, Sanggye Paik Hospital, Inje University College of Medicine Seoul, Korea, Republic of, 139-707 Department of Neurology, Korea University Guro Hospital Seoul, Korea, Republic of, 152-703 Department of Neurology, Ewha Womans University Mokdong Hospital Seoul, Korea, Republic of, 158-710 Collapse <<
NCT02904109	Healthy	Phase 2	Completed	-	Switzerland ... more >> University of Basel, Division of Cognitive Neuroscience Basel, Switzerland, 4055 Collapse <<
NCT02321852	Healthy	Phase 2	Completed	-	Switzerland ... more >> University of Basel, Division of Cognitive Neuroscience Basel, Switzerland, 4055 Collapse <<

Triflusal/三氟柳 Catalog No. CSN16812

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