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Tirofiban

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Chemical Structure| 144494-65-5 同义名 : L700462;MK383
CAS号 : 144494-65-5
货号 : A167431
分子式 : C22H36N2O5S
纯度 : 99%+
分子量 : 440.597
MDL号 : MFCD05237246
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

1M HCl: 50 mg/mL(113.48 mM)，配合低频超声，并调节pH至1
动物实验配方：
生物活性
靶点

  • Integrin
描述 The binding of glycoprotein (GP) IIb/IIIa receptor to fibrinogen is a prerequisite in platelet activation and aggregation. Tirofiban is a potent GPIIb/IIIa antagonist. It inhibited the aggregation of in vitro human gel-filtered platelets induced by ADP, collagen, gamma-thrombin, and U46619 with IC50 values ranging from 12 nM to 31 nM. It also displayed inhibitory activity against human PRP platelet aggregation induced by ADP, collagen, gamma-thrombin, U46619, epinephrine, and arachidonic acid with IC50 values ranging from 31 nM to 66 nM. Tirofiban inhibited the platelet aggregation in human, rhesus monkey, and dog whole blood with IC50 values of 81, 140, and 353 nM, respectively. The intravenous administration of tirofiban (1 mg/kg) in dogs significantly inhibited ex vivo ADP-induced platelet aggregation in platelet-rich plasma (PRP) and the prolongation of template bleeding time. Continuous infusions of tirofiban (0.1-10 µg/kg/min) inhibited ex vivo platelet aggregation in PRP induced by ADP and collagen in a dose-dependent manner. Moreover, the combined treatment with tirofiban (1µg/kg/min, i.v., 120min) and ticlopidine (20 mg/kg/day, p.o., 4 days) in dogs did not change the pharmacokinetic profile of tirofiban nor the platelet count[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
NCT01087723 - Completed - -
NCT01087723 Acute Coronary Syndrome Phase 3 Completed - -
NCT01103440 Stable Angina Phase 2 Completed - United States, New York ... 展开 >> Mount Sinai Medical Center New York, New York, United States, 10029 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.13mL

22.70mL

4.54mL

2.27mL
参考文献

[1]van 't Hof AW, Valgimigli M. Defining the role of platelet glycoprotein receptor inhibitors in STEMI: focus on tirofiban. Drugs. 2009;69(1):85-100.

[2]Hartman GD, Egbertson MS, et al. Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors. J Med Chem. 1992 Nov 27;35(24):4640-2.

[3]Tirofiban (Aggrastat®)