8001-27-2

Basic information

• Product Name: HIRUDIN
• Synonyms: hirudex;recombinanthirudin;HIRUDIN RECOMBINANT;DESULFATO-HIRUDIN;DESULFO-HIRUDIN;[63-TYROSINE]HIRUDIN (HV1), LEECH;NATIVE HIRUDIN;[TYR63]HIRUDIN (HV1), LEECH
• CAS NO: 8001-27-2
• Molecular Formula: C287H440N80O113S7
• Molecular Weight: 7043.4877
• EINECS: 232-279-1
• Product Categories: Coagulation Proteins and ReagentsPlasma&Blood Proteins;HirudinProtease Inhibitors;Plasma&Blood Proteins;Plasma, Blood, and Related Proteins and Reagents;Protease Inhibitor Specificity Index;Proteins and Derivatives;R to;Thrombin;ThrombinEnzyme Inhibitors by Enzyme;proteins
• Mol File: 8001-27-2.mol
• Article Data: 0

Chemical Properties

• Appearance: white/lyophilized powder
• Storage Temp.: −70°C
• Merck: 13,4737
• CAS DataBase Reference: HIRUDIN(CAS DataBase Reference)
• NIST Chemistry Reference: HIRUDIN(8001-27-2)
• EPA Substance Registry System: HIRUDIN(8001-27-2)

Safety Data

• Safety Statements: 22-24/25
• WGK Germany: 3
• RTECS: MR8440000
• F: 10-21
• Hazardous Substances Data: 8001-27-2(Hazardous Substances Data)

Usage

Description

Hirudin, also known as Refludan, is a potent, specific, and almost irreversible inhibitor of thrombin, originally isolated from the saliva of leeches (Hirudo medicinalis). The gene for recombinant hirudin was synthesized and expressed in Saccharomyces cerevisiae, resulting in a protein that differs from the native protein by the first two amino acids (Leu1 and Thr2) and has Tyr63 not sulfated, while retaining the three disulfide bonds. It forms a 1:1 complex with thrombin, binding to the active catalytic site and the anion binding exosite (fibrinogen binding cleft). Hirudin has several advantages over heparin, including its ability to inhibit thrombin bound to extracellular matrices, not requiring antithrombin III as a cofactor, not being inhibited by activated platelets, not increasing platelet activity, and being a pure, single compound with a single mechanism of action.

Uses

Used in Pharmaceutical Industry:
Hirudin is used as an anticoagulant for the treatment of heparin-associated thrombocytopenia, myocardial infarcts, unstable angina, and cardiovascular events. It offers several advantages over heparin, such as not being inhibited by activated platelets and not increasing platelet activity.
Used in Research Applications:
Recombinant hirudin from yeast is used as an inhibitor in mannan-binding lectin serine protease 2 (MASP2) activation assays, providing a specific and potent tool for studying the activity of MASP2 in various biological processes.
Used in Platelet Adhesion Assays:
Hirudin is used as a pre-treatment for nanosheets in phosphate-buffered saline (PBS) to study platelet adhesion, providing a controlled environment to investigate the interactions between platelets and various surfaces.

Originator

Hoechst Merion Roussel (Germany)

Biochem/physiol Actions

The anticoagulant, hirudin, is the most potent natural inhibitor of both soluble and clot-bound thrombin. It forms a high-affinity 1:1 complex with thrombin, occluding both the proteolytic site and exosite I (fibrinogen and PAR recognition site). Hirudin blocks thrombus growth and platelet activation, and has been suggested as the clinically preferred anticoagulant (over heparin and citrate) for its specific mode of action and absence of side effects. It is not metabolized in the bloodstream of humans and is eliminated unchanged via kidney filtration.