Argatroban Impurity 23

Argatroban-d₃ is intended for use as an internal standard for the quantification of argatroban by GC- or LC-MS. Argatroban is a reversible inhibitor of thrombin (IC₅₀s = 0.01 and 0.09 μM for the free and clot-bound forms, respectively). It is selective for thrombin over factor Xa, trypsin, plasmin, and tissue plasminogen activator (K_is = 0.0045, 53, 0.19, 25.7, and 87.7 μM, respectively). It inhibits thrombin-induced platelet aggregation in washed isolated guinea pig platelets with an IC₅₀ value of 0.077 μM. Argatroban (3.2 mg/kg, s.c.) decreases thrombus formation in a guinea pig model of iron chloride-induced arterial thrombosis. Formulations containing argatroban have been used in the prevention or treatment of thrombosis in patients with heparin-induced thrombocytopenia.

Labelled synthetic thrombin inhibitor. Antithrombotic.

[1] HEE DONG PARK . Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug[J]. Bioorganic & Medicinal Chemistry Letters, 2013, 23 17: Pages 4779-4784. DOI: 10.1016/j.bmcl.2013.07.008
[2] YASUKO KATO . Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig[J]. European journal of pharmacology, 2003, 473 2: Pages 163-169. DOI: 10.1016/s0014-2999(03)01973-3