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编 号:F158488
分子式:C22H37ClN2O5S
分子量:477.06
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生物活性:
Tirofiban (L700462) hydrochloride is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.

体内研究:
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.Tirofiban hydrochloride (60 μg/kg; i.v.; once) enhances eNOS activity, decreases iNOS activity and reduces area of no-reflow after reperfusion following AMI.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.Animal Model:Male Sprague-Dawley rats (10 to 15-week-age; 270-330 g).
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)
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%.

体外研究:
Tirofiban hydrochloride (0.25, 1, 3 μg/mL; 72 hours) increases proliferation of HAEC cells.Tirofiban hydrochloride (24 hours) closes the scratch of HUVECs migration within 18 hours.Tirofiban hydrochloride (0.25, 1 μg/mL; 1 hour) induces production of VEGF after 30 minutes which can stimulates proliferation of endothelial cells.
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