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

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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
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 Information & 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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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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