Tirofiban (L700462) hydrochloride 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 hydrochloride 可通过诱导 VEGF 的产生来刺激内皮细胞的迁移和增殖。Tirofiban hydrochloride 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) hydrochloride is a selective and reversible plateletintegrinreceptor (Gp IIb/IIIa) antagonist that inhibitsfibrinogenbinding to this receptor and has antithrombotic activity. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production ofVEGF. Tirofiban hydrochloride 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 hydrochloride (0.25, 1, 3 μg/mL; 72 hours) increases proliferation of HAEC cells[1].
Tirofiban hydrochloride (24 hours) closes the scratch of HUVECs migration within 18 hours[1].
Tirofiban hydrochloride (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 hydrochloride (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 hydrochloride (60 μg/kg; i.v.; once) enhances eNOS activity, decreases iNOS activity and reduces area of no-reflow after reperfusion following AMI[2].
Tirofiban hydrochloride (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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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