Tirofiban (L700462) 是一种选择性和可逆性的血小板整合素受体 (Gp IIb/IIIa) 拮抗剂，能抑制纤维蛋白原与该受体结合，具有抗血栓活性。Tirofiban 可通过诱导 VEGF 的产生来刺激内皮细胞的迁移和增殖。Tirofiban 可通过缓解缺血区的心肌微血管结构和内皮功能障碍显著减少心肌无回流和缺血再灌注损伤，从而改善心脏功能。
| 生物活性 | Tirofiban (L700462) is a selective and reversible plateletintegrinreceptor (Gp IIb/IIIa) antagonist that inhibitsfibrinogenbinding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production ofVEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area[1][2][3]. |
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体外研究
(In Vitro) | Tirofiban (0.25, 1, 3 μg/mL; 72 hours) increases proliferation of HAEC cells[1].
Tirofiban (24 hours) closes the scratch of HUVECs migration within 18 hours[1].
Tirofiban (0.25, 1 μg/mL; 1 hour) induces production of VEGF after 30 minutes which can stimulates proliferation of endothelial cells[1].
Cell Proliferation Assay[1] | Cell Line: | HAEC cells | | Concentration: | 0.25, 1, 3 μg/mL | | Incubation Time: | 72 hours | | Result: | Increased proliferation of HAEC cells. |
Cell Migration Assay[1] | Cell Line: | HUVEC cells | | Concentration: | | | Incubation Time: | 24 hours | | Result: | Stimulated the migratory capacity of endothelial cells. |
Western Blot Analysis[1] | Cell Line: | HAEC cells | | Concentration: | 0.05, 0.12, 0.25, 1 μg/mL | | Incubation Time: | 1 hour | | Result: | Induced production of VEGF which stimulated proliferation of endothelial cells. |
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体内研究
(In Vivo) | Tirofiban (60 μg/kg; i.v.; once) shows activity of increasing contraction force, ventricular compliance, and improving heart function by increasing HR, LVESP, dp/dtmax, and reducing LVEDP[2].
Tirofiban (60 μg/kg; i.v.; once) enhances eNOS activity, decreases iNOS activity and reduces area of no-reflow after reperfusion following AMI[2].
Tirofiban (50 μg/per; irrigate; once) shows anticoagulant effect with patency rates of 59% at 24 hours after microvascular anastomosis in the crush model[3].
| Animal Model: | Male Sprague-Dawley rats (10 to 15-week-age; 270-330 g)[2]. | | Dosage: | 60 μg/kg | | Administration: | Intravenous injection; once. | | Result: | Increased contraction force, ventricular compliance, and improved heart function.
Reduced the size of no-reflow and infarct. |
| Animal Model: | Sprague-Dawley rats (350-400 g; crush injury model)[3] | | Dosage: | 50 μg/per (50 μg/mL, 1 mL for each) | | Administration: | Irrigate 1 mL within the vessel lumen (before placement of the last suture); once. | | Result: | Showed anticoagulant effect with patency rates of 59%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: 1M HCl : 50 mg/mL(113.48 mM;ultrasonic and adjust pH to 1 with HCl) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) DMSO :< 1 mg/mL (ultrasonic;warming)(insoluble or slightly soluble) 配制储备液 | 1 mM | 2.2696 mL | 11.3482 mL | 22.6963 mL | | 5 mM | 0.4539 mL | 2.2696 mL | 4.5393 mL | | 10 mM | 0.2270 mL | 1.1348 mL | 2.2696 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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