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H0393 Sigma-Aldrich

Hirudin

recombinant, expressed in unspecified host, ≥7,000 ATU/mg protein (ATU = antithrombin units)

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Description

Application

Antithrombotic efficacy by parenteral route is substantially prolonged by incorporation into cationic liposomes, which act as a sort of sustained-release device.

Physical properties

The anticoagulant hirudin is a ~7 kDa acidic protein containing 65 amino acid residues. It occurs naturally in leeches (Hirudo medicinalis). It is the most potent natural inhibitor of both soluble and clot-bound thrombin. Hirudin binds thrombin with high affinity and covers more than 20% of the surface area of thrombin, occluding both the active site and exosite I (fibrinogen and PAR recognition site). This coverage blocks thrombus growth and platelet activation. Hirudin is not metabolized in the bloodstream of humans and is eliminated unchanged via kidney filtration. Native hirudin contains a sulfated tyrosyl residue (Tyr63), three disulfide bridges, and a high proportion of dicarboxylic acids. Hirudin is not glycosylated, and lacks tryptophan, arginine, and methionine residues. At least 20 isoforms have been identified and sequenced.

This recombinant hirudin product corresponds to the HV-1 variant sequence, with the exception that the Tyr63 residue is not sulfated.

Unit Definition

One antithrombin unit (ATU) will neutralize one NIH unit of thrombin at 37 °C, based on direct comparison to an NIH thrombin reference standard.

Reconstitution

Hirudin is soluble in water. The literature cites the use of "Dilution Fluid II" (35.7 mM acetic acid, 35.7 mM sodium diethyl barbiturate, 0.85% NaCl, 1% bovine serum albumin, and 0.5% PEG, pH 7.4) to dissolve hirudin (500 ATU/mL) and thrombin. Hirudin is reported to be soluble in pyridine, but practically insoluble in alcohol, ether, acetone, or benzene.

Analysis Note

Protein determined by Lowry.

Safety & Documentation

Safety Information

Personal Protective Equipment 
RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Certificate of Origin (COO)

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Protocols & Articles

Articles

Plasma Derived Proteins and Enzymes

Despite their complexity, blood and plasma are abundant biological resources for the discovery of drug targets and biomarkers for human disease. It is estimated that plasma may contain as many as 40,...
BioFiles 2006, 1.5, 2.
Keywords: Applications, Gas chromatography, Type

Peer-Reviewed Papers
15

References

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