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  3. Tirofiban

Tirofiban (Synonyms: L700462; MK383)

Cat. No.: HY-17369B Purity: 98.37%
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Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.

For research use only. We do not sell to patients.

Tirofiban Chemical Structure

Tirofiban Chemical Structure

CAS No. : 144494-65-5

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Description

Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. 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].

IC50 & Target

Gp IIb/IIIa Receptor[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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%.
Clinical Trial
Molecular Weight

440.60

Formula

C22H36N2O5S

CAS No.
SMILES

O=S(N[[email protected]](C(O)=O)CC1=CC=C(OCCCCC2CCNCC2)C=C1)(CCCC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : < 1 mg/mL (ultrasonic;warming) (insoluble or slightly soluble)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

Purity & Documentation
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Tirofiban
Cat. No.:
HY-17369B
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