|2-(4-(1-氧代-2-异吲哚啉基)苯基)丁酸|CsnPharm

CAS No.: 63610-08-2

吲哚布芬 Catalog No. CSN21951

Synonyms: Ibustrin;K 3920;吲哚布芬

Indobufen is a platelet aggregation inhibitor and a reversible cyclooxygenase inhibitor. It has been used in studying the supportive care and prevention of Atrial Fibrillation.

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400-920-2911

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技术信息

生物活性

描述Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes. Indobufen prevents TF expression and activity both in isolated and in whole blood monocytes. Reduction of TxA2 synthesis, coupled with a lack of effect on PGE2 levels and prevention of ERK1/2 phosphorylation are highlighted as the mechanisms through which indobufen negatively affects TF^[1]. Intragastric-administrated indobufen can significantly reduce the APTT (activated partial thromboplastin time), PT (prothrombin time), TT (thrombin time), PF3 (platelet factor 3,4), FI, II, V, VIII, and X (the coagulation factor 1, 2, 5, 8, 10) plasma contents. Its inhibitory effect on plasma FII was better than thrombin inhibitor dabigatran with effect on FX better than FXa inhibitor rivaroxaban^[2]. Indobufen has been shown to be as effective as aspirin plus dipyridamole in preventing the reocclusion of coronary and femoro-popliteal artery bypass grafts and has been shown to significantly reduce platelet deposition on haemodialysis membranes^[3].
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
NCT01232023	Healthy	Phase 1	Unknown	-	Korea, Republic of ... more >> Pusan National University Yangsan Hospital Recruiting Pusan, Korea, Republic of Contact: Sangmin Choe, M.D., Ph.D. 82-55-360-1732 Asan Medical Center Recruiting Seoul, Korea, Republic of Contact: Hyeong-Seok Lim, M.D., Ph.D. 82-2-3010-4613 Principal Investigator: Hyeong-Seok Lim, M.D., Ph.D. Collapse <<
NCT03230851	Coronary Atherosclerosis	Phase 4	Not yet recruiting	August 10, 2018	China, Jiangsu ... more >> First Affiliated Hospital of Nanjing Medical University Nanjing, Jiangsu, China, 210029 Collapse <<
NCT00244426	Atrial Fibrillation	Phase 3	Completed	-	-

参考文献

[1] Eligini S, Violi F, Banfi C, Barbieri SS, Brambilla M, Saliola M, Tremoli E, Colli S. Indobufen inhibits tissue factor in human monocytes through a thromboxane-mediated mechanism. Cardiovasc Res. 2006 Jan;69(1):218-26
[2] Liu J, Xu D, Xia N, Hou K, Chen S, Wang Y, Li Y. Anticoagulant Activities of Indobufen, an Antiplatelet Drug. Molecules. 2018 Jun 15;23(6):1452
[3] Wiseman LR, Fitton A, Buckley MM. Indobufen. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in cerebral, peripheral and coronary vascular disease. Drugs. 1992 Sep;44(3):445-64

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
- 3.3860 mL
- 16.9301 mL
- 33.8601 mL
- 5 mM
- 0.6772 mL
- 3.3860 mL
- 6.7720 mL
- 10 mM
- 0.3386 mL
- 1.6930 mL
- 3.3860 mL

技术信息

CAS号

63610-08-2

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H17NO3

运输

蓝冰

分子量

295.33

别名

Ibustrin;K 3920;吲哚布芬

溶解度

DMSO	215.0 mg/mL (728.0 mM)
Water	insoluble

动物实验配方

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