Background and Overview of Eptifibatide

Eptifibatide is an artificially synthesized cyclic peptide containing one mercaptopropionic acid and six amino acid residues. It is a targeted platelet glycoprotein GPIIb/IIIa receptor antagonist that selectively and reversibly inhibits the final common pathway of platelet aggregation (plasma coagulation is caused by the binding of coagulation factor I to GP IIb/IIIa), and can reverse ischemic status caused by thrombosis.

Eptifibatide is mainly used in clinical practice to treat unstable angina and acute myocardial infarction. Its main adverse reaction is bleeding, with most bleeding being mild to moderate. The main bleeding site is the site of vascular puncture during PCI, and cerebral hemorrhage is rare. Eptifibatide was first developed by the American company COR Therapeuties and was first launched in the United States under the trade name "IIItegreliII" in July 1998.

Pharmacological effects of Epitibatide acetate

Eptifibatide is a synthetic cyclic peptide. Its structure is surrounded by 7 amino acids, and its molecular formula contains 6 amino acids and a phthalein residue. There is an active group in the molecular formula of Epitibatide: lysine glycine aspartic acid. This active group can bind to the IIb/IIIa receptor on platelet glycoprotein, blocking the IIb/la receptor and preventing clotting factor I from binding to the IIb/la receptor on platelet glycoprotein.

Due to the fact that one clotting factor 1 can bind to two IIb/la receptors (multiple IIb/IIIa receptors on one platelet can bind to multiple clotting factor I), the binding of clotting factor I to IIb/IIIa receptors results in platelet bridging, leading to platelet aggregation. However, only one Eptifibatide molecule can bind to one IIb/IIIa receptor, and the result of Eptifibatide binding to IIb/IIla receptors is to "block" the IIb/IIIa receptor's anti platelet aggregation effect.

The selectivity of Eptifibatide towards IIb/III receptors is high. The inhibitory effect of Epitibatide on platelet glycoprotein LIIb/IIIa receptors is competitive, and the inhibitory effect is stronger when the concentration of Eptifibatide is higher. The binding of Eptifibatide to IIb/ma receptors is reversible, and the effect of Eptifibatide is halved 4 hours after discontinuation.

Eptifibatide acetate CAS:188627-80-7 Omizzur lab in stock 

Preparation of Eptifibatide acetate

Step 1: Preparation of Fmoc-Pro-Cys (Trt) resin

Step 2: Preparation of Fomc-Trp (boc) - Pro-Cys (Trt) resin

Step 3: Preparation of Fomc-Asp (OtBu) - Trp (boc) - Pro-Cys (Trt) resin

Step 4: Preparation of Mpr (trt) - Har (pbf) - Gly-Asp (OtBu) - Trp (boc) - Pro-Cys (Trt) resin

Step 5: Preparation of Reduced Eptifibatide 

Step 6: Preparation of crude Eptifibatide acetate

Step 7: Purification, salt transfer, concentration, and freeze-drying of Eptifibatide 

Shipping

Usually we arrange shipping within 24 hours of receiving the order (except Sundays). We ship by Fedex, DHL ,EMS and other methods for global shipping. Most countries can deliver goods within 7 days.

Storage

When peptides are received, please make sure they are kept in a cool, dark place. For best storage, store them under fridge at 4°C or colder, away from bright light. Solid peptides are stable at room temperature for a few weeks. For long-term storage, -20°C is best.

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