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IntegratorsIntegrelin Intrifiban L-Cysteinamide,N6-(aminoiminomethyl)-N2- (3-mercapto-1-oxopropyl)-L-lysylglycyl-L-Raspartyl- L-tryptophyl-L-prolyl-,cyclic (1f6)-disulfide
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Product introduction:
Description | Eptifibatide is a reversible antagonist of the glycoprotein llb/llla complex, a specific platelet adhesion receptor that plays a central role in the cascade of thrombus formation by allowing mediators such as fibrinogen or von Willbrand factor to cross-link adjacent platelets and to give rise to aggregation. In diverse animal experimental models of arterial thrombosis, treatment with Eptifibatide resulted in an enhanced lysis of occlusive thrombus and a restoration of arterial blood flow. In clinical trials involving patients with acute coronary syndromes, Eptifibatide demonstrated a significant decrease in the incidence of death or nonfatal myocardial infarction at 30 days. In other trials in patients undergoing percutaneous coronary intervention (PCI), it showed a positive trend. Eptifibatide has the advantage of being short acting, its antiplatelet effect being rapidly reversible. |
Originator | Cor Therapeutics (US) |
Uses | Eptifibatide is a cyclical heptapeptide with anticoagulant activity. Eptifibatide selectively and reversibly binds to and blocks the platelet glycoprotein IIb/IIIa receptor. This prevents the binding of fibrinogen, von Willebrand factor, and other adhesive ligands and leads to an inhibition of platelet aggregation and prevents thrombus development. It is an efficient peptide drug to reduce the risk of cardiac ischemic events, however has a short half-life. Therefore, antithrombotic agents like eptifibatide are required to become improved with a protected and targeted delivery system such as using nano-liposomes to the site of thrombus. |
Definition | ChEBI: Eptifibatide is a synthetic homodetic cyclic peptide comprising N(alpha)-(3-sulfanylpropanoyl)homoarginyl, glycyl, aspartyl, tryptophyl, prolyl and cysteinamide residues connected in sequence and cyclised via a disulfide bond. Derived from a protein found in the venom of the southeastern pygmy rattlesnake, Sistrurus miliarus barbouri, eptifibatide is an anti-coagulant that inhibits platelet aggregation by selectively blocking the platelet glycoprotein IIb/IIIa receptor, so preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. It is used in the management of unstable angina and in patients undergoing coronary angioplasty and stenting procedures. It has a role as a platelet aggregation inhibitor and an anticoagulant. It is an organic disulfide, a macrocycle and a homodetic cyclic peptide. |
Brand name | Integrilin |
General Description | Eptifibatide (188627-80-7) is a syntheticcyclic heptapeptide that acts as a GPIIb/IIIa receptor antagonist,thus causing inhibition of platelet aggregation. Itsstructure is based on the natural product barbourin, a peptideisolated from the venom of a pygmy rattlesnake (Sistrurusmilarud barbouri). As part of the structure, there is a sequenceRGD that can bind to the RGD receptor found onplatelets and block its ability to bind with fibrinogen. Thisagent is used in the treatment of unstable angina and for angioplasticcoronary interventions. |
Biological Activity | Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation. Eptifibatide prevents binding of the adhesion proteins fibrinogen and von Willebrand factor to GPIIb/IIIa on the surface of activated platelets to prevent aggregation and thrombus formation. It inhibits ADP-induced citrated blood aggregation (IC50 = 0.11-0.22 μg/ml) in vitro and in vivo (IC50 = 52 μg/ml in porcine plasma). Formulations containing eptifibatide have been used to reduce risk of thrombolysis in myocardial infarction in patients undergoing percutaneous coronary intervention. |
Mechanism of action | Eptifibatide reversibly inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor and other adhesive ligands to the glycoprotein (GP) IIb/IIIa receptors. When administered intravenously, eptifibatide inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner. www.accessdata.fda.gov |
Clinical Use | Eptifibatide is a cyclic heptapeptide composed of six amino acids and one mercaptopropionyl residue. The cyclization is completed via a disulfide linkage between the cysteine and the mercaptopropionyl moieties. The lysine-glycine-aspartate component of eptifibatide is highly specific for the GPIIb/IIIa receptor, with low binding affinity, as indicated by the rapid dissociation constant. Because of this, eptifibatide is a reversible, parenterally administered antagonist of platelet aggregation. |
Drug interactions | Potentially hazardous interactions with other drugs Iloprost: increased risk of bleeding. |
Metabolism | Renal excretion accounts for approximately 50% of total body clearance of eptifibatide; approximately 50% of the amount cleared is excreted unchanged in the urine. |
storage | Store at -20°C |
Our company specializes in processing and selling chemical raw materials, chemical products, pharmaceutical intermediates, veterinary medicine intermediates, dye intermediates, pigments, cosmetics raw materials and chemical reagents,
Our company has a number of sales team, service and information feedback vertical integration of a sound marketing network, products are sold throughout the country and exported to South Asia, Europe, America, Africa and other more than 20 countries and regions.
Companies adhering to the "pursuit of quality, innovation and development" business philosophy, to serve as a foundation, for the survival by the quality, seek development by science and technology, adhere to quilty comes first,fair price,good sense of customer service and responsibility. in the future hebei Nengqian import and export trade Co.,Ltd will always hold "integrity, innovation" business philosophy, to achieve honesty management, on the way of specialization, internationalization, Keep moving!
Our advantages:
1, High quality with competitive price:
1) Standard:BP/USP/EP/Enterprise standard
2) All Purity≥99%
3) We are manufacturer and can provide high quality products with factory price.
2, Fast and safe delivery
1) Parcel can be sent out in 24 hours after payment.Tracking number available
2) Secure and discreet shipment.Various transportation methods for your choice.
3) Customs pass rate ≥99%
4) We have our own agent/remailer/distributor who can help us ship our products very fast and safe,
and we have stock in there for transferring.
Product Packaging:
1) 1kg/bag (1kg net weight, 1.1kg gross weight, packed in an aluminum foil bag)
2) 25kg/drum (25kg net weight, 28kg gross weight; Packed in a cardboard-drum with two plastic-bags inside; Drum Size: 510mm high, 360mm diameter)
Storage:
Stored in a cool and dry well-closed container. Keep away from moisture and strong light/heat.
Delivery:
Usually within3-5 working days after full payment.
transport:
EMS,DHL, TNT, UPS ,FEDEX, BY AIR, BY SEA
DHL Express, FedEx and EMS for quantity less than 50KG, usually called as DDU service;
Sea shipping for quantity over 500KG; And air shipping is available for 50KG above;
For high value products, please select air shipping and DHL express for safe;
Our Service:
1. Fast Delivery: We can delivery within 24 hours upon receipt of your payment.
2. Quality can be promised. Hot sell to Worldwide.
3. Payment Terms: T/T,, t/t
4. Free Sample available at any time.
5. Tracking your order at any time. Inform your order's further new situation at any time.
6. Package: Professional packing with professional materials.
FAQ:
1.Are you a trade company or factory
We are a factory with our own trading company.
2.How do you control the quality
Our factory is equipped with professional technicians to control quality, out inspectors take sample for testing every 2 hours to ensure the quality of our production. We also accept BV, SGS or any other Third-party inspection.
3.How long is lead time
We deliver goods within 3 days for small order, 7-10 days for bulk order.
4. Where is your factory located How can I visit the factory
Our factory located in HEBEI, China.
5.Can i get some samples
Yes, we can supply free sample, but the shipping cost be paid by our customers.
6.How to start orders or make payments
Proforma invoice will be sent first after confirmation of order, enclosed our bank information.Payment by T/T,
7. How to confirm the Product Quality before placing orders
You can get free samples for some products,you only need to pay the shipping cost or arrange a courier to us and take the samples.
8. How long is lead time
We deliver goods within 3 days for small order, 7-10 days for bulk order.
9. How do you treat quality complaint
First of all, our quality control will reduce the quality problem to near zero. If there is a realquality problem caused by us, we will send you free goods for replacement or refund your loss.
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