Eptifibatide Human

Eptifibatide Human
Cat. No.
BT28948
Source
Synonyms
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity
Greater than 98.0% as determined by:
(a) Analysis by RP-HPLC.
(b) Analysis by SDS-PAGE.
Usage
Prospec's products are furnished for LABORATORY RESEARCH USE ONLY. The product may not be used as drugs, agricultural or pesticidal products, food additives or household chemicals.
Shipped with Ice Packs
In Stock

Description

Synthetic Eptifibatide is a 6 amino acid peptide having a MW of 832.5 Dalton the following sequence Mpr-Har-Gly-Asp-Trp-Pro-Cys-NH2.

Product Specs

Introduction
Eptifibatide is a cyclic peptide, derived from a protein found in the venom of the southeastern pygmy rattlesnake, that inhibits platelet aggregation. It achieves this by binding to the glycoprotein (GP) IIb/IIIa receptor on human platelets. As an arginin-glycin-aspartat-mimetic, it demonstrates reversible binding to platelets.
Description
Synthetic Eptifibatide is a hexapeptide with a molecular weight of 832.5 Daltons. Its amino acid sequence is: Met-Pro-Har-Gly-Asp-Trp-Pro-Cys-NH2.
Physical Appearance
White, sterile-filtered powder in lyophilized (freeze-dried) form.
Formulation
The lyophilization process of Eptifibatide does not involve any additives.
Solubility
For reconstitution of lyophilized Eptifibatide, it is recommended to use sterile 18MΩ-cm H2O at a minimum concentration of 100 µg/ml. This solution can be further diluted with other aqueous solutions.
Stability
Lyophilized Eptifibatide exhibits stability at room temperature for up to 3 weeks; however, for extended storage, it should be stored in a desiccated environment below -18°C. After reconstitution, Eptifibatide should be stored at 4°C for 2-7 days. For long-term storage, freezing at -18°C is recommended. The addition of a carrier protein (0.1% HSA or BSA) is suggested for long-term storage. Repeated freeze-thaw cycles should be avoided.
Purity
The purity of this product is greater than 98.0%, determined by: (a) Reverse-phase high-performance liquid chromatography (RP-HPLC) analysis and (b) Sodium dodecyl-sulfate polyacrylamide gel electrophoresis (SDS-PAGE) analysis.

Product Science Overview

Mechanism of Action

Eptifibatide works by reversibly binding to the platelet receptor glycoprotein IIb/IIIa, which is crucial for platelet aggregation . By blocking this receptor, eptifibatide prevents the binding of fibrinogen, von Willebrand factor, and other adhesive ligands, thereby inhibiting platelet aggregation in a dose- and concentration-dependent manner .

Clinical Uses

Eptifibatide is primarily used to reduce the risk of acute cardiac ischemic events, such as death and myocardial infarction, in patients with unstable angina or non-ST-segment elevation myocardial infarction (NSTEMI) . It is often administered in conjunction with aspirin or clopidogrel and heparin (either low molecular weight or unfractionated) . Additionally, it is used as an adjunct to percutaneous coronary intervention (PCI) to prevent complications during and after the procedure .

Pharmacokinetics

Eptifibatide has a relatively short half-life of approximately 2.5 hours and is primarily excreted through the kidneys . It has a bioavailability of around 25% when administered intravenously .

Development and Approval

Eptifibatide was developed by Millennium Pharmaceuticals and is marketed under the brand name Integrilin . It has gained broad acceptance as the third inhibitor of glycoprotein IIb/IIIa, following the specific antibody abciximab and the non-peptide tirofiban .

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