For research use only.
Catalog No.S3085 Synonyms: MK-383
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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|Description||Tirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.|
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. 
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.  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. 
-  Hartman GD, et al. J Med Chem, 1992, 35(24), 4640-4642
-  Egbertson MS, et al. J Med Chem, 1994, 37(16), 2537-2551.
-  Lynch JJ Jr, et al. J Pharmacol Exp Ther, 1995, 272(1), 20-32.
|In vitro||DMSO||0.005 mg/mL (0.01 mM)|
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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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