Name: Tirofiban
Brand: Selleck Chemicals
SKU: S3085
Availability: InStock
Rating: 5 (1 reviews)

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

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COA
NMR
HPLC
SDS
Datasheet

99.28

Related Targets	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Bcr-Abl Actin FAK Kinesin
Other Integrin Inhibitors	SB273005 Cilengitide trifluoroacetate Cilengitide (EMD 121974) RGD peptide (Arg-Gly-Asp) ATN-161 Cyclo(-RGDfK) TFA Cyclo(RGDyK) TFA Leukadherin-1 A-205804 Pyrintegrin

Solubility

In vitro
Batch:

5%TFA : 3.02 mg/mL

DMSO : 0.005 mg/mL (0.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.15mg/ml (0.34mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	440.6	Formula	C₂₂H₃₆N₂O₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	144494-65-5	Download SDF Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	MK-383			Smiles	CCCCS(=O)(=O)NC(CC1=CC=C(C=C1)OCCCCC2CCNCC2)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	GPIIb/IIIa
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. This compound 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.
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. When administered to humans at 0.15μg/kg/min for 4 h, this compound produced a 2.5-fold increase in bleeding time and 97% inhibition of ADP-induced platelet aggregation.
References	[1] http://www.ncbi.nlm.nih.gov/pubmed?term=1469694 [2] http://www.ncbi.nlm.nih.gov/pubmed?term=8057299 [3] https://eresources.library.mssm.edu/login?url=http://www.ncbi.nlm.nih.gov/pubmed?term=7815334 [4] http://www.ncbi.nlm.nih.gov/pubmed?term=7955799 [5] http://www.ncbi.nlm.nih.gov/pubmed?term=8403299

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Tirofiban Integrin antagonist

Chemical Structure

Molecular Weight: 440.6