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Argatroban

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Argatroban Basic information
Argatroban Chemical Properties
  • Melting point:188-1890C
  • Boiling point:777.2±70.0 °C(Predicted)
  • Density 1.47±0.1 g/cm3(Predicted)
  • storage temp. Store at +4°C
  • pka10.44±0.40(Predicted)
  • form White to off-white powder.
  • CAS DataBase Reference74863-84-6(CAS DataBase Reference)
Argatroban Usage And Synthesis
  • DescriptionArgatroban is a new synthetic antithrombotic agent useful in maintenance anticoagulation them ischemic stroke and disseminated intravascular coagulation. In patients on hemodialysis, argatroban is su enor to heparin, generating a more stable antithrombin effect. Other potential uses include progressing ischemic stroke and disseminated intravascular coagulation.
  • Chemical PropertiesWhite to Off-White Crystalline Solid
  • OriginatorMitsubishi Kasei; Daiichi (Japan)
  • UsesSynthetic thrombin inhibitor. Antithrombotic.
  • Usesanticoagulant;direct thrombine inhibitor
  • brand nameNovastan (Mitsubishi Chemical Corporation, Japan);Slonnon.
  • PharmacokineticsArgatroban is administered subcutaneously because of the low lipophilicity of the drug. The drug is bound to plasma protein and is metabolized via CYP3A4/5 to the aromatized metabolite and the two hydroxylated metabolites. The M-1 metabolite retains 20 to 30% of the antithrombotic activity. Coadministration of argatroban with inhibitors of CYP3A4 does not appear to produce clinically significant effects. Argatroban is eliminated via biliary secretion into the feces.
  • Clinical UseArgatroban has been approved for the prophylaxis and treatment of thrombosis in patients with HIT (79). Argatroban is a peptidomimetic that binds selectively to the catalytic site of thrombin as a univalent competitive DTI. Argatroban is available as a mixture of 21-R and 21-S diastereomers (64:36), with the S-isomer approximately twice as potent as the R-isomer. The drug is a reversible inhibitor of both free thrombin as well as clot-bound thrombin.
Argatroban Preparation Products And Raw materials
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