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    Tirofiban (L700462; MK383)
    Tirofiban (L700462; MK383)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1599
    CAS #: 144494-65-5 Purity ≥98%

    Description: Tirofiban (formerly known as L-700462; MK-383; L700462; MK383; Aggrastat) is a novel non-peptide antagonist of glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) that has been approved for use as an antiplatelet drug. Tirofiban is a small molecule inhibitor of the protein-protein interaction between fibrinogen and the platelet integrin receptor GP IIb/IIIa and is the first drug candidate whose origins can be traced to a pharmacophore-based virtual screening lead. Tirofiban Hydrochloride is the hydrochloride salt form of tirofiban, a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation. It is more soluable than Tirofiban. Tirofiban inhibits platelet aggregation of gel-filtered platelets induced by 10 μM ADP with IC50 of 9 nM, but the IC50 for inhibition of human umbilical vein adhesion to vitronectin, which depends on ɑvβ3 vitronectin receptors, is 62 μmol/L.

    References: J Med Chem. 1992 Nov 27;35(24):4640-2; Clin Pharmacol Ther. 1994 Oct;56(4):377-88.

    Related CAS#: 150915-40-5 (HCl hydrate); 142373-60-2 (HCl); 144494-65-5 (free base)

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    Molecular Weight (MW)440.6
    FormulaC22H36N2O5S
    CAS No.144494-65-5 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: <1 mg/mL
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILESO=C(O)[[email protected]](CC1=CC=C(OCCCCC2CCNCC2)C=C1)NS(=O)(CCCC)=O
    SynonymsMK-383 Hydrochloride; Aggrastat; L-700462; MK-383; L 700462; MK 383; L700462; L-700,462; MK383


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    In Vitro

    In vitro activity: Tirofiban (MK-383, Aggrastat) is a nonpeptide derivative of tyrosine that selectively inhibits the GP-IIb/IIIa receptor, with minimal effects on the ɑvβ3 vitronectin receptor. It inhibits platelet aggregation of gel-filtered platelets induced by 10 μM ADP with IC50 of 9 nM, but the IC50 for inhibition of human umbilical vein adhesion to vitronectin, which depends on ɑvβ3 vitronectin receptors, is 62 μmol/L.


    Kinase Assay: Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist IC50 value: Target: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation. Tirofiban is an antithrombotic used in the treatment of unstable angina. Tirofiban, in a concentration-dependent manner reduced platelet aggregation evoked by ADP (IC50 approximately 70 ng/ml), collagen (IC50 approximately 200 ng/ml), and thrombin (IC50 approximately 5,000 ng/ml).

    In VivoTirofiban (10 to 500 mg/kg or 360-min continuous i.v. infusions of 1 to 10 micrograms/kg/min) inhibits platelet aggregation responses to ADP and collagen in canine models. When administered to humans at 0.15μg/kg/min for 4 h, Tirofiban produced a 2.5-fold increase in bleeding time and 97% inhibition of ADP-induced platelet aggregation.  
    Animal modelAdult mongrel dogs 
    Formulation & DosageDissolved in saline; 500 mg/kg; i.p. injection 
    ReferencesJ Med Chem. 1992 Nov 27;35(24):4640-2; Clin Pharmacol Ther. 1994 Oct;56(4):377-88.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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