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抑制剂/激动剂
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/ 整合素 / Tirofiban/替罗非班

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

货号：A167431 同义名： L700462; MK383

Tirofiban是一种选择性、可逆性的血小板整合素受体 (Gp IIb/IIIa) 拮抗剂，通过抑制纤维蛋白原与受体结合，发挥抗血栓作用，同时可改善缺血再灌注损伤并促进心脏功能恢复。

Tirofiban/替罗非班 化学结构 CAS号：144494-65-5
Tirofiban/替罗非班 化学结构
CAS号：144494-65-5
Tirofiban/替罗非班 3D分子结构
CAS号：144494-65-5
Tirofiban/替罗非班 化学结构 CAS号：144494-65-5
Tirofiban/替罗非班 3D分子结构 CAS号：144494-65-5
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Tirofiban/替罗非班 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]}
批次查询： 批次纯度:

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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/替罗非班 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/替罗非班 细胞实验

Cell Line
Concentration Treated Time Description References
Human platelets 0.0172 +0.0071 µM (IC50) 2 min Inhibited arachidonic acid-induced platelet aggregation Br J Pharmacol. 2001 Aug;133(8):1396-404
Human platelets 0.0242 +0.0049 µM (IC50) 2 min Inhibited collagen-induced platelet aggregation Br J Pharmacol. 2001 Aug;133(8):1396-404
Human platelets 0.0115 +0.0015 µM (IC50) 2 min Inhibited ADP-induced platelet aggregation Br J Pharmacol. 2001 Aug;133(8):1396-404
C3H10T1/2 cells 50 µM 24 hours TF reduced triglyceride content in lipid droplets and altered lipid droplet distribution from large to small droplets. Cell Biosci. 2022 Jan 28;12(1):10
M2 polarized macrophages 1 μg/ml 48 hours Tirofiban, by blocking β3 integrin, reversed the spike-induced M2 to M1 morphological and functional switch, including reduced CD80 expression increase and CD206 expression decrease, and inhibited STAT1 activation. Heliyon. 2024 Jul 31;10(15):e35341
Human platelets 10 nM to 2 µM 5 minutes Evaluate the inhibitory effect of Tirofiban on ADP-induced platelet aggregation, showing concentration-dependent inhibition. Drug Des Devel Ther. 2016 Sep 21;10:2989-2996
Mouse platelets 30 nM 5 minutes To evaluate the inhibitory effect of Tirofiban on ADP-induced mouse platelet aggregation, results showed that 30 nM Tirofiban had limited effect on mouse platelet aggregation. Circulation. 2011 Jan 25;123(3):319-26
Human platelets 30 nM 5 minutes To evaluate the inhibitory effect of Tirofiban on ADP-induced human platelet aggregation, results showed that 30 nM Tirofiban significantly inhibited platelet aggregation. Circulation. 2011 Jan 25;123(3):319-26

Tirofiban/替罗非班 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats Deep venous thrombosis model Intravenous injection 0.6 mg/kg (unlabeled Tirofiban) or 2.0 nmol (99mTc-Tirofiban) Single dose Evaluate the ability of 99mTc-Tirofiban to detect deep venous thrombosis in vivo, showing accumulation at the thrombus site for early detection. Drug Des Devel Ther. 2016 Sep 21;10:2989-2996
VWFR1326H mutant mice Laser-injured arteriole thrombosis model Intravenous injection 25 μg/kg intravenous bolus followed by 0.15 μg/kg/min continuous infusion Single bolus followed by continuous infusion for approximately 15 minutes To evaluate the inhibitory effect of Tirofiban on human platelet-mediated thrombus formation in VWFR1326H mutant mice, results showed that Tirofiban significantly reduced thrombus formation area. Circulation. 2011 Jan 25;123(3):319-26
Mice High-fat diet-induced obesity model Intraperitoneal injection 50 µg/kg Once daily for 2 weeks TF reduced body weight gain and white adipose tissue weight in high-fat diet mice, upregulated ILK expression and activity, and altered the expression of adipogenesis and lipid metabolism markers. Cell Biosci. 2022 Jan 28;12(1):10

Tirofiban/替罗非班 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/替罗非班 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/替罗非班 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/替罗非班 技术信息

CAS号144494-65-5
分子式C22H36N2O5S
分子量 440.6
SMILES Code O=C(O)[C@H](CC1=CC=C(C=C1)OCCCCC2CCNCC2)NS(=O)(CCCC)=O
MDL No. MFCD05237246
别名 L700462; MK383
运输蓝冰
InChI Key COKMIXFXJJXBQG-NRFANRHFSA-N
Pubchem ID 60947
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C
溶解方案

1M HCl: 50 mg/mL(113.48 mM)，配合低频超声，并调节pH至1

Tags: Tirofiban | 144494-65-5 | L700462 | MK383 | L 700462 | L-700462 | MK383 | MK 383 | MK-383 | Gp IIb/IIIa Receptor Antagonist | Cytoskeleton | Integrin | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Tirofiban/替罗非班 纯度/质量文件 | Tirofiban/替罗非班 亚型比较 | Tirofiban/替罗非班 生物活性 | Tirofiban/替罗非班 临床数据 | Tirofiban/替罗非班 参考文献 | Tirofiban/替罗非班 实验方案 | Tirofiban/替罗非班 技术信息

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