Tirofiban

For research use only.

Catalog No.S3085 Synonyms: MK-383

1 publication

Tirofiban Chemical Structure

CAS No. 144494-65-5

Tirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.

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Selleck's Tirofiban has been cited by 1 publication

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Biological Activity

Description Tirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.
Targets
GPIIb/IIIa [1]
In vitro

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. [1][2] 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. [2]

In vivo

Tirofiban (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. [3] 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. [4][5]

Protocol

Solubility (25°C)

In vitro DMSO 0.005 mg/mL (0.01 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 440.6
Formula

C22H36N2O5S

CAS No. 144494-65-5
Storage powder
in solvent
Synonyms MK-383
Smiles CCCCS(=O)(=O)NC(CC1=CC=C(C=C1)OCCCCC2CCNCC2)C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03797729 Recruiting Drug: Tirofiban|Drug: Normal saline ST Elevation Myocardial Infarction Shanghai Zhongshan Hospital May 14 2019 Phase 4
NCT03048019 Unknown status Drug: Tirofiban|Drug: Cangrelor Non-ST Elevation Myocardial Infarction (NSTEMI) Inova Health Care Services August 23 2017 --
NCT01766154 Completed Drug: Tirofiban Renal Insufficiency Medicure January 2013 Phase 1
NCT01336348 Completed Drug: Prasugrel|Drug: Tirofiban ST Segment Elevation Myocardial Infarction Università degli Studi di Ferrara April 2010 Phase 3
NCT00407771 Unknown status Drug: Tirofiban Coronary Artery Disease Jordan Hospital|Merck Sharp & Dohme Corp. November 2007 Phase 4
NCT00538317 Completed Drug: tirofiban Acute Myocardial Infarction Hospices Civils de Lyon July 2007 Phase 4

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Integrin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID