Bioactivity | Tirofiban (L700462) hydrochloride monohydrate 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 monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate 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]. |
Target | Gp IIb/IIIa Receptor |
Invitro | Tirofiban hydrochloride monohydrate (0.25, 1, 3 μg/mL; 72 hours) increases proliferation of HAEC cells[1].Tirofiban hydrochloride monohydrate (24 hours) closes the scratch of HUVECs migration within 18 hours[1].Tirofiban hydrochloride monohydrate (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: |
In Vivo | Tirofiban hydrochloride monohydrate (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 monohydrate (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 monohydrate (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: |
Name | Tirofiban hydrochloride monohydrate |
CAS | 150915-40-5 |
Formula | C22H39ClN2O6S |
Molar Mass | 495.07 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Giordano A, et al. Tirofiban induces VEGF production and stimulates migration and proliferation of endothelial cells. Vascul Pharmacol. 2014 May-Jun;61(2-3):63-71. [2]. Liu X, et al. Effects of tirofiban on the reperfusion-related no-reflow in rats with acute myocardial infarction. J Geriatr Cardiol. 2013 Mar;10(1):52-8. [3]. Yates YJ, et al. The effect of tirofiban on microvascular thrombosis: crush model. Plast Reconstr Surg. 2005 Jul;116(1):205-8 |