Desirudin

Desirudin (CGP 39393) is a thrombin inhibitor. Desirudin can inhibit the formation of blood clots and venous stasis thrombosis, which is used for the research of thrombocytopenia or platelet dysfunction[1][2].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Thrombin

ED50: 0.01 mg/kg (i.v.) and 0.45 mg/kg (s.c.)[2].

Desirudin (CGP 39393, 0.75-3.0 mg/kg, a bolus plus infusion administration, dogs model of cardiopulmonary bypass) is effective in Inhibiting clot formation[1]. Desirudin (0.01-1 mg/kg approximately, Intravenous injections and subcutaneous injection, rat shunt model) inhibits thrombus development with ED50 values of 0.3 mg/kg (i.v.) and 1.0 mg/kg (s.c.), and inhibits venous stasis thrombosis with ED50 values of 0.01 mg/kg (i.v.) and 0.45 mg/kg (s.c.)[2]. Animal Model: Male mongrel dogs model of cardiopulmonary bypass[1] Dosage: 1.0 mg/kg + 0.75 mg/kg/h, 1.0 mg/kg + 1.50 mg/kg/h, 1.0 mg/kg + 2.25 mg/kg/h, 1.0 mg/kg + 3.0 mg/kg/h. Administration: Administered as a bolus plus infusion Result: Inhibits clot formation with no adverse hemodynamic or hematologic effects. Animal Model: Rat shunt model of thrombus formation on a cotton-thread[2] Dosage: 0.01-1 mg/kg approximately Administration: Intravenous injections, subcutaneous injection Result: Inhibited thrombus development with ED50 values of 0.3 mg/kg (i.v.) and 1.0 mg/kg (s.c.). Inhibited venous stasis thrombosis with ED50 values of 0.01 mg/kg (i.v.) and 0.45 mg/kg (s.c.).

[1]. J M Walenga, et al. Evaluation of CGP 39393 as the Anticoagulant in Cardiopulmonary Bypass Operation in a Dog Model. Ann Thorac Surg. 1994 Dec;58(6):1685-9.

[2]. M D Talbot, et al. Recombinant desulphatohirudin (CGP 39393) anticoagulant and antithrombotic properties in vivo. Thromb Haemost. 1989 Feb 28;61(1):77-80.