Tirofiban

Catalog No.S3085 Synonyms: MK-383

For research use only.

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

Tirofiban Chemical Structure

CAS No. 144494-65-5

Selleck's Tirofiban has been cited by 1 Publication

Purity & Quality Control

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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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 440.6
Formula

C22H36N2O5S

CAS No. 144494-65-5
Storage 3 years -20°C powder
2 years -80°C in solvent
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 Unknown status 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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