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  4. Tirofiban

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.

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CAS No. : 144494-65-5

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Based on 6 publication(s) in Google Scholar

Other Forms of Tirofiban:

Tirofiban Related Antibodies

Top Publications Citing Use of Products

    Tirofiban purchased from MedChemExpress. Usage Cited in: Microsyst Nanoeng. 2026 Jan 1;12(1):7.  [Abstract]

    Anti-aggregation efficiency of single-drug combinations for platelets in the combinatorial screening tests for Volunteer 1. For Aspirin (Asp), the concentrations were 2 μM, 4 μM (2 μM + 2 μM), 20 μM, 22 μM (2 μM + 20 μM), and 40 μM (20 μM + 20 μM). For Tirofiban (Tif), the concentrations were 0.2 μM, 0.4 μM (0.2 μM + 0.2 μM), 2 μM, 2.2 μM (0.2 μM + 2 μM), and 4 μM (2 μM + 2 μM). For Ticagrelor, the concentrations were 1 μM, 2 μM (1 μM + 1 μM), 10 μM, 11 μM (10 μM + 1 μM), and 20 μM (10 μM + 10 μM). The results showed that 4 μM Tif (Tirofiban) exhibited the strongest platelet aggregation inhibition.

    Tirofiban purchased from MedChemExpress. Usage Cited in: Am J Respir Cell Mol Biol. 2025 Feb 28.  [Abstract]

    CCK8 analysis indicated that the proliferation effect of PH-PLT-EC CM on PASMCs was diminished by Tirofiban (30 μg/mL) or eptifibatide (10 μg/mL). MFI = mean fluorescence intensity.

    Tirofiban purchased from MedChemExpress. Usage Cited in: Am J Respir Cell Mol Biol. 2025 Feb 28.  [Abstract]

    Treatment with GPIIb/IIIa antagonists Tirofiban (30 or 300 μg/mL; 45 min) or eptifibatide (1; 10 μg/mL) decreased platelet–EC adhesion. Platelet adhesion was measured by quantifying the remaining fluorescence intensity after the unattached platelets were removed.

    Tirofiban purchased from MedChemExpress. Usage Cited in: Am J Respir Cell Mol Biol. 2025 Feb 28.  [Abstract]

    The conditioned medium from EC–platelet cocultures treated with Tirofiban (30 μg/mL), eptifibatide (10 μg/mL), or A-205804 (250 μmol/L) showed reduced PDGF-BB levels.

    Tirofiban purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 February 01.

    RGD-integrin selectivity of lassotides 36-38 and conjugates 47-49 (shaded), as measured by competitive inhibition vs LAP in ELISA assays against integrins αvβ3, αvβ6 and αvβ8 (as described above) and αvβ1, αvβ5, αIIbβ3, α5β1, and α8β1. *MK-042948 was used as a positive control for all integrin assays except αIIbβ3, where Tirofiban49 was employed.

    View All Integrin Isoform Specific Products:

    View All Isoforms
    αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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]
    Cellular Effect
    Cell Line Type Value Description References
    HUVEC IC50
    100 μM
    Compound: 17
    Inhibition of HUVEC attachment to human vitronectin
    Inhibition of HUVEC attachment to human vitronectin
    		[PMID: 1469694]
    HUVEC IC50
    260 μM
    Compound: 17
    Inhibition of HUVEC attachment to human fibrinogen
    Inhibition of HUVEC attachment to human fibrinogen
    		[PMID: 1469694]
    HUVEC IC50
    > 300 μM
    Compound: 17
    Inhibition of HUVEC attachment to human fibronectin
    Inhibition of HUVEC attachment to human fibronectin
    		[PMID: 1469694]
    Platelet IC50
    0.03 μM
    Compound: Tirofiban
    Antiplatelet activity in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation by Born's method
    Antiplatelet activity in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation by Born's method
    		[PMID: 26912112]
    Platelet IC50
    0.032 μM
    Compound: Tirofiban
    Inhibition of ADP-induced human platelet aggregation in platelet-rich plasma by Born's method
    Inhibition of ADP-induced human platelet aggregation in platelet-rich plasma by Born's method
    		[PMID: 23757209]
    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].

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

    Tirofiban Related Antibodies

    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].

    MedChemExpress (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%.
    Molecular Weight

    440.60

    Formula

    C22H36N2O5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S(N[C@H](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: 

    1M HCl : 50 mg/mL (113.48 mM; ultrasonic and adjust pH to 1 with HCl)

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

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2696 mL 11.3482 mL 22.6963 mL
    5 mM 0.4539 mL 2.2696 mL 4.5393 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    1M HCl 1 mM 2.2696 mL 11.3482 mL 22.6963 mL 56.7408 mL
    5 mM 0.4539 mL 2.2696 mL 4.5393 mL 11.3482 mL
    10 mM 0.2270 mL 1.1348 mL 2.2696 mL 5.6741 mL
    15 mM 0.1513 mL 0.7565 mL 1.5131 mL 3.7827 mL
    20 mM 0.1135 mL 0.5674 mL 1.1348 mL 2.8370 mL
    25 mM 0.0908 mL 0.4539 mL 0.9079 mL 2.2696 mL
    30 mM 0.0757 mL 0.3783 mL 0.7565 mL 1.8914 mL
    40 mM 0.0567 mL 0.2837 mL 0.5674 mL 1.4185 mL
    50 mM 0.0454 mL 0.2270 mL 0.4539 mL 1.1348 mL
    60 mM 0.0378 mL 0.1891 mL 0.3783 mL 0.9457 mL
    80 mM 0.0284 mL 0.1419 mL 0.2837 mL 0.7093 mL
    100 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5674 mL
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    Tirofiban Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Tirofiban144494-65-5L700462 MK383L 700462L-700462MK383MK 383MK-383IntegrinACSsAMINRHUVECHAECVEGFantithromboticInhibitorinhibitorinhibit

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