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替罗非班 /Tirofiban {[allProObj[0].p_purity_real_show]}

货号:A167431 同义名: L700462;MK383

Tirofiban is a non-peptide reversible antagonist of the platelet integrin glycoprotein (GP) IIb/IIIa receptor used as an antiplatelet drug.

Tirofiban 化学结构 CAS号:144494-65-5
Tirofiban 化学结构
CAS号:144494-65-5
Tirofiban 3D分子结构
CAS号:144494-65-5
Tirofiban 化学结构 CAS号:144494-65-5
Tirofiban 3D分子结构 CAS号:144494-65-5
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Tirofiban 纯度/质量文件 产品仅供科研

货号:A167431 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Integrin 其他靶点 纯度
Tirofiban 99%+
ATN-161 98%
RGD 98%
A-205804 ++

E-selectin, IC50: 20 nM

ICAM-1, IC50: 25 nM

98%
SB-273005 ++++

αvβ5 receptor, IC50: 0.3 nM

αvβ3 receptor, IC50: 1.2 nM

98+%
Lifitegrast 97%
Cilengitide TFA +++

αvβ5 receptor, IC50: 79 nM

αvβ3 receptor, IC50: 4.1 nM

99%+
Cyclo(-RGDfK) TFA 99%+
Cyclo(RGDyK) trifluoroacetate ++

αVβ3 integrin, IC50: 20 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Tirofiban 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].

Tirofiban 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 <<

Tirofiban 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®)

Tirofiban 实验方案

计算器
存储液制备 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

Tirofiban 技术信息

CAS号144494-65-5
分子式C22H36N2O5S
分子量 440.597
别名 L700462;MK383
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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