Eptifibatide monoacetate | CAS No. 1248559-53-6

Description

Product Description

Eptifibatide monoacetate (CAS 1248559-53-6) is a potent cyclic heptapeptide known for its role as a competitive antagonist of the platelet glycoprotein IIb/IIIa receptor (GP IIb/IIIa, integrin αIIbβ3). This receptor is a critical mediator of platelet aggregation, and its blockade results in significant anti-platelet activity, making Eptifibatide monoacetate a key research compound for studying cardiovascular and thrombotic disorders.

Background

Platelets play a fundamental role in hemostasis and thrombosis. Under vascular injury conditions, platelets adhere to exposed subendothelial structures and become activated, leading to conformational changes in GP IIb/IIIa receptors. These receptors then bind fibrinogen, von Willebrand factor, and other ligands, bridging platelets together to form aggregates. Excessive platelet aggregation can cause arterial thrombosis, leading to life-threatening conditions such as myocardial infarction and ischemic stroke.

Eptifibatide monoacetate mimics natural ligands of GP IIb/IIIa but acts as a reversible competitive inhibitor, preventing fibrinogen binding and subsequent platelet cross-linking.

Research Significance

• Cardiovascular Research – Widely studied in models of acute coronary syndrome (ACS), percutaneous coronary intervention (PCI), and ischemic stroke.

• Thrombosis Studies – Used to examine the role of GP IIb/IIIa inhibition in preventing arterial clot formation.

• Platelet Biology – Serves as a research tool to dissect pathways of platelet adhesion, aggregation, and signaling.

• Drug Discovery – Provides a framework for the design of novel antiplatelet therapeutics.

Structural Features

• Cyclic Heptapeptide: The cyclic structure confers stability and high receptor affinity.

• Specificity: Selectively binds to activated GP IIb/IIIa receptors.

• Reversibility: Antagonism is reversible, providing safety advantages in experimental use.

Advantages as a Research Tool

• Mimics clinical-grade inhibitors of GP IIb/IIIa.

• Facilitates mechanistic studies of platelet aggregation.

• Serves as a model compound for anti-thrombotic therapy development.

Product Specifications

Notes

• HPLC and MS validated.

• Endotoxin-free preparation available.

• Packaged in sterile, secure containers for laboratory use.

Mechanism of Action

Eptifibatide monoacetate acts by blocking the platelet GP IIb/IIIa receptor (integrin αIIbβ3), which is the final common pathway for platelet aggregation.

• Competitive Antagonism
  Eptifibatide binds to activated GP IIb/IIIa receptors, preventing fibrinogen from bridging platelets together.

• Inhibition of Platelet Cross-Linking
  By disrupting fibrinogen and von Willebrand factor binding, platelet-to-platelet adhesion is significantly reduced.

• Reversibility
  Unlike some irreversible inhibitors, Eptifibatide monoacetate binds reversibly, which enhances safety in dynamic research models.

• Downstream Effects
  The blockade of platelet aggregation reduces thrombus formation in vascular injury models, supporting research into anti-thrombotic strategies.

This mechanism highlights Eptifibatide monoacetate as an indispensable peptide tool for cardiovascular and thrombosis research.

Side Effects

Research Observations

• Bleeding Risk: Expected due to platelet aggregation inhibition.

• Reversibility: Reduced long-term bleeding compared to irreversible antagonists.

• Thrombocytopenia: Rare, but observed in platelet studies.

Limitations

• Effective concentrations must be carefully determined for each experimental model.

• Cytotoxicity is generally low but must be validated in mammalian studies.

Precautions

• Not for human use.

• Should be handled with standard laboratory safety protocols.

Disclaimer

All information is intended for laboratory research use only. Eptifibatide monoacetate is not approved for human use, medical treatment, or diagnostic purposes.

Keywords

Eptifibatide monoacetate, CAS 1248559-53-6, cyclic heptapeptide, platelet GP IIb/IIIa antagonist, antiplatelet peptide, thrombosis research peptide, cardiovascular peptide, platelet aggregation inhibitor.

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