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Tirofiban hydrochloride monohydrate

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Chemical Structure| 150915-40-5 同义名 : 盐酸替罗非班 一水合物 ;L700462 hydrochloride monohydrate;MK383 hydrochloride monohydrate;Tirofiban (hydrochloride hydrate);MK-383 Hydrochloride;Tirofiban Hydrochloride
CAS号 : 150915-40-5
货号 : A662355
分子式 : C22H39ClN2O6S
纯度 : 98%
分子量 : 495.073
MDL号 : MFCD07368623
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(212.09 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：

PO 0.5% CMC-Na 31 mg/mL suspension

生物活性
描述 The binding of glycoprotein (GP) IIb/IIIa receptor to fibrinogen is a prerequisite in platelet activation and aggregation. Tirofiban Hydrochloride Monohydrate is the hydrochloride monohydrate form of Tirofiban. 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 Acute Coronary Syndrome Phase 3 Completed - -
NCT01087723 - 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

2.02mL

0.40mL

0.20mL

10.10mL

2.02mL

1.01mL

20.20mL

4.04mL

2.02mL
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]Winter JP, Juergens CP. The role of tirofiban in the management of coronary artery disease. Cardiovasc Hematol Disord Drug Targets. 2008 Jun;8(2):138-46.

[3]Tirofiban (Aggrastat®)