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Indobufen

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Chemical Structure| 63610-08-2 同义名 : Ibustrin;K 3920
CAS号 : 63610-08-2
货号 : A397716
分子式 : C18H17NO3
纯度 : 97%
分子量 : 295.332
MDL号 : -
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(846.5 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.39mL

0.68mL

0.34mL

16.93mL

3.39mL

1.69mL

33.86mL

6.77mL

3.39mL
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