Bivalirudin

Bivalirudin
Cat. No.
BT28850
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.
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Description

The active of Bivalirudin substance is a synthetic 20 amino acid peptide. The amino acid sequence is Phe-Pro-Arg-Pro-Gly-Gly-Gly-Gly- Asn-Gly-Asp-Phe-Glu-Glu-Ile- Pro-Glu-Glu-Tyr-Leu. The Mw is 2180 dalton.

Product Specs

Introduction
Bivalirudin is a direct thrombin inhibitor that exhibits specificity for both the catalytic site and the anion-binding exosite of thrombin, effectively targeting both circulating and clot-bound forms. Its mechanism of action involves reversible binding to thrombin. As a serine protease, thrombin plays a crucial role in the coagulation cascade. It catalyzes the conversion of fibrinogen to fibrin monomers and activates Factor XIII to Factor XIIIa, facilitating the formation of a stable fibrin clot through covalent cross-linking. Moreover, thrombin activates Factors V and VIII, amplifying thrombin generation. Additionally, it induces platelet activation, leading to aggregation and granule release.
Description
Bivalirudin is a synthetic peptide composed of 20 amino acids, with a molecular weight of 2180 Daltons. Its amino acid sequence is as follows: Phe-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu.
Physical Appearance
White, sterile-filtered powder obtained through lyophilization.
Formulation
The lyophilized formulation contains 1 mg/ml of Bivalirudin, along with 0.5 mg of Mannitol and 50 µg of sodium hydroxide as excipients, with a pH of 5.5.
Solubility
To reconstitute lyophilized Bivalirudin, it is recommended to dissolve it in sterile 18 MΩ-cm H2O at a concentration of at least 100 µg/ml. The resulting solution can be further diluted using other aqueous solutions.
Stability
Lyophilized Bivalirudin demonstrates stability at room temperature for a period of 3 weeks. However, it is recommended to store it desiccated at a temperature below -18°C. After reconstitution, Bivalirudin should be stored at 4°C for a duration of 2 to 7 days. For long-term storage, freezing at -18°C is recommended. It is advisable to add a carrier protein such as HSA or BSA (0.1%) for enhanced stability during long-term storage. Repeated freeze-thaw cycles should be avoided.
Purity
The purity of Bivalirudin is greater than 98.0%, as determined by the following analytical methods: Reverse-Phase High-Performance Liquid Chromatography (RP-HPLC) and Sodium Dodecyl Sulfate-Polyacrylamide Gel Electrophoresis (SDS-PAGE).

Product Science Overview

Chemical Structure and Properties

Bivalirudin is a 20-amino acid peptide with the chemical formula C98H138N24O33 and a molar mass of approximately 2180.317 g/mol . It is a synthetic analog of hirudin, a naturally occurring anticoagulant found in the saliva of the medicinal leech Hirudo medicinalis . The structure of bivalirudin allows it to bind specifically and reversibly to thrombin, inhibiting its activity.

Mechanism of Action

Bivalirudin works by directly inhibiting thrombin, an enzyme that plays a crucial role in the blood coagulation process . Thrombin converts fibrinogen into fibrin, which forms the structural basis of blood clots. By binding to thrombin, bivalirudin prevents the formation of fibrin and, consequently, blood clots . This mechanism is particularly useful during PCI procedures, where the risk of clot formation is high.

Clinical Uses

Bivalirudin is used in various clinical settings, including:

  • Percutaneous Coronary Intervention (PCI): It is administered to patients undergoing PCI to prevent clot formation during the procedure .
  • Acute Coronary Syndromes: Bivalirudin is used in patients with unstable angina or non-ST segment elevation myocardial infarction (NSTEMI) who are at moderate to high risk and are planned for PCI .
  • Heparin-Induced Thrombocytopenia (HIT): It is also indicated for patients with HIT, a condition where heparin administration leads to a decrease in platelet count and an increased risk of thrombosis .
Pharmacokinetics

Bivalirudin is administered intravenously, and its effects are immediate. It has a short half-life of approximately 25 minutes in patients with normal renal function . The drug is cleared from the plasma through a combination of renal mechanisms and proteolytic cleavage .

Advantages and Limitations

One of the significant advantages of bivalirudin over other anticoagulants, such as heparin, is its ability to inhibit thrombin directly and reversibly . This property reduces the risk of bleeding complications and allows for more precise control of anticoagulation. However, bivalirudin can cause blood stagnation, so it is essential to monitor hematocrit, activated partial thromboplastin time (aPTT), international normalized ratio (INR), and blood pressure during its administration .

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