Home Neuronal Signaling P2 Receptor antagonist Prasugrel

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Prasugrel P2 Receptor antagonist

Cat.No.S1258

Prasugrel (Effient, Efient, Prasita,CS-747, LY640315,PCR 4099) is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events.
Prasugrel P2 Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 373.44

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 373.44 Formula

C20H20FNO3S

 Storage (From the date of receipt)
CAS No. 150322-43-3 Download SDF Storage of Stock Solutions

Synonyms Effient, Efient, Prasita,CS-747, LY640315,PCR 4099 Smiles CC(=O)OC1=CC2=C(S1)CCN(C2)C(C3=CC=CC=C3F)C(=O)C4CC4

Solubility

In vitro
Batch:

DMSO : 33 mg/mL (88.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

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Mechanism of Action

Targets/IC50/Ki
P2Y12 receptor [1]
In vitro

This compound is a novel orally active thienopyridine with faster, higher and more reliable inhibition of platelet aggregation than clopidogrel reflecting its metabolism in vivo to an active metabolite with selective P2Y(12) antagonistic activity. [1]
In vivo

Prasugrel shows platelet inhibition that was 8.2 times more potent than clopidogrel in WT mice. [1] This compound (3 and 10 mg/kg) dose-relatedly and significantly reduces thrombus-mediated cerebral infarction 24 hours after the irradiation in rat models of cerebral and peripheral arterial occlusive diseases. It (0.3-3 mg/kg) reduces incidence, total area, and total number of cerebral infarcts in a dose-related manner 24 hours after the vascular injury in an embolic infarction rats model. This chemical (0.03-3 mg/kg/day) administered from the day before the lauric acid injection for 11 successive days inhibits the progression of the disease in a dose-related manner in rats with lauric acid-induced peripheral arterial occlusive diseases. [2] It administrated in dogs (0.03-0.3 mg/kg/day) and monkeys (0.1 and 0.3 mg/kg/day) once a day for 14 days results in potent, dose-related and cumulative inhibition of ADP-induced platelet aggregation. This compound (0.1-1 mg/kg/day, p.o.) significantly prolongs the time to arterial occlusion and increases the duration of arterial patency in a rat model of electrically-induced arterial thrombosis. [3]
References

Applications

Methods Biomarkers Images PMID
Western blot p-VEGDFR2 / VEGFR2 / p-STAT3 / STAT3 / p-p65 / p65 / p-AKT / AKT / p-ERK / ERK S1257-WB2 28383032

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05774431 Recruiting
Acute Myocardial Infarction
University Hospital Heidelberg|AstraZeneca
 March 13 2023 --
NCT05053828 Completed
Type2 Diabetes|Antiplatelet Drugs|Myocardial Infarction|Heart Failure
Tabula Rasa HealthCare
 September 20 2021 --
NCT04471870 Completed
Acute Coronary Syndrome
Chiesi Farmaceutici S.p.A.
 October 23 2020 --

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