Tirofiban

Synonyms: MK-383

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

Tirofiban Chemical Structure

Tirofiban Chemical Structure

CAS: 144494-65-5

Selleck's Tirofiban has been cited by 1 publication

Purity & Quality Control

Batch: S308501 5%TFA] 3.02 mg/mL] false] DMSO] 0.005 mg/mL] false] Water] Insoluble] false Purity: 99.28%
99.28

Choose Selective Integrin Inhibitors

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
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
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]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05793671 Not yet recruiting STEMI Assiut University April 1 2023 Not Applicable
NCT03797729 Unknown status ST Elevation Myocardial Infarction Shanghai Zhongshan Hospital May 14 2019 Phase 4
NCT01766154 Completed Renal Insufficiency Medicure January 2013 Phase 1
NCT01336348 Completed ST Segment Elevation Myocardial Infarction Università degli Studi di Ferrara April 2010 Phase 3
NCT00407771 Unknown status Coronary Artery Disease Jordan Hospital|Merck Sharp & Dohme LLC November 2007 Phase 4
NCT00538317 Completed Acute Myocardial Infarction Hospices Civils de Lyon July 2007 Phase 4

Chemical lnformation & Solubility

Molecular Weight 440.6 Formula

C22H36N2O5S

CAS No. 144494-65-5 SDF Download Tirofiban SDF Download Tirofiban SDF
Smiles CCCCS(=O)(=O)NC(CC1=CC=C(C=C1)OCCCCC2CCNCC2)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

5%TFA : 3.02 mg/mL

DMSO : 0.005 mg/mL ( (0.01 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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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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