Description

Product Description

SKF 106760 (CAS 126053-71-2) is a potent and selective glycoprotein IIb/IIIa (GP IIb/IIIa) receptor antagonist, acting as a powerful inhibitor of platelet aggregation and thrombus formation. The GP IIb/IIIa receptor plays a critical role in platelet cross-linking by fibrinogen during clot formation, and its inhibition provides a direct mechanism to prevent arterial thrombosis. SKF 106760 has been demonstrated to exert significant antiplatelet and antithrombotic activity in multiple preclinical studies, including canine models of carotid artery stenosis.

Unlike conventional antiplatelet drugs such as aspirin, SKF 106760 operates by directly blocking fibrinogen binding sites on the GP IIb/IIIa receptor, thereby inhibiting the final common pathway of platelet aggregation. This makes it an important pharmacological tool for investigating platelet function, thrombosis mechanisms, and potential therapeutic strategies for aspirin-resistant thrombi.

Research Applications

SKF 106760 is widely used in cardiovascular and hematological research, with applications including:

• Evaluation of platelet aggregation mechanisms in vitro and in vivo.

• Investigation of GP IIb/IIIa receptor antagonism in animal thrombosis models.

• Study of antithrombotic efficacy in conditions of vascular stenosis.

• Exploration of aspirin-resistant thrombus elimination.

• Comparison of novel antiplatelet agents with established GP IIb/IIIa antagonists.

Because of its reliable pharmacodynamics, SKF 106760 provides researchers with a reproducible model for studying both physiological and pathological thrombosis processes.

Product Specifications

Mechanism of Action

The glycoprotein IIb/IIIa receptor (integrin αIIbβ3) is the final common pathway for platelet aggregation, facilitating fibrinogen-mediated cross-linking of platelets to form a thrombus. SKF 106760 acts as a competitive antagonist at this receptor, thereby preventing the binding of fibrinogen and other adhesive ligands such as von Willebrand factor (vWF).

1. Inhibition of Platelet Aggregation

By occupying the GP IIb/IIIa receptor binding site, SKF 106760 effectively prevents platelet aggregation induced by various agonists, including ADP, thrombin, collagen, and arachidonic acid. This results in profound inhibition of platelet plug formation.

2. Prevention of Thrombus Formation

In animal models of arterial injury and stenosis, SKF 106760 prevents platelet-rich thrombus formation. Studies in dogs have shown its ability to inhibit thrombus development in stenotic carotid arteries and to eliminate pre-formed, aspirin-resistant thrombi.

3. Superior to Traditional Antiplatelet Agents

Unlike aspirin or P2Y12 inhibitors, SKF 106760 blocks the final step of platelet aggregation, offering a broader inhibitory spectrum. It can therefore serve as a benchmark compound for evaluating the efficacy of novel GP IIb/IIIa inhibitors or other antithrombotic agents.

4. Pharmacodynamic Profile

SKF 106760 shows dose-dependent inhibition of platelet aggregation in vitro and in vivo. In canine studies, significant inhibition was observed at micromolar concentrations, with rapid onset and reversible effects upon compound removal.

Through its targeted action on GP IIb/IIIa, SKF 106760 serves as a valuable research-grade standard compound for exploring cardiovascular disease mechanisms, drug resistance, and clot biology.

Side Effects

As an experimental compound not approved for clinical use, SKF 106760’s adverse reactions are observed primarily in preclinical studies. Laboratory findings include:

• Prolonged bleeding time due to platelet function inhibition.

• Dose-dependent inhibition of hemostasis in vivo.

• Possible hypotension or mild vascular reactions in animal models.

• Transient thrombocytopenia with repeated high-dose administration.

• Potential interaction with other antiplatelet agents, increasing bleeding risk in combined experimental setups.

Proper handling and dosage control are essential in laboratory conditions to avoid excessive inhibition of platelet function or unwanted hemorrhagic events.

Disclaimer

For research use only. Not intended for human or veterinary use. Handle with appropriate laboratory safety measures.

Keywords

SKF 106760, CAS 126053-71-2, glycoprotein IIb/IIIa antagonist, platelet aggregation inhibitor, fibrin receptor blocker, antithrombotic agent, cardiovascular research compound, thrombosis inhibitor, integrin αIIbβ3 ligand, aspirin-resistant thrombi, platelet function modulator.wholesale peptides.

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