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Description: Argatroban (MD-805; MCI-9038; Argipidine) is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM. Argatroban is used as an anticoagulant that acts as a direct thrombin inhibitor. Argatroban received FDA approval in 2000 for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT). As a direct thrombin inhibitor, Argatroban reversibly binds to the thrombin active site. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions which include fibrin formation, activation of coagulation factors V, VIII, and XIII; activation of protein C, and platelet aggregation as well.
References: Br J Pharmacol. 1994 Dec;113(4):1209-14; Jpn J Pharmacol. 1995 Oct;69(2):143-8.
Related CAS #: 141396-28-3 (hydrate); 74863-84-6 (anhydrous);
Chemical Name: (2R,4R)-4-methyl-1-(((3-methyl-1,2,3,4-tetrahydroquinolin-8-yl)sulfonyl)-L-arginyl)piperidine-2-carboxylic acid
SMILES Code: O=C(O)[[email protected]]1C[[email protected]](C)CCN1C([[email protected]](CCCNC(N)=N)NS(=O)(C2=CC=CC3=C2NCC(C)C3)=O)=O
Exact Mass: 508.2468
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: Argatroban is a potent and selective synthetic thrombin inhibitor with Ki values against thrombin ranging from 5 nM to 39 nM. Argatroban has antithrombotic properties in a wide variety of animal models of both platelet-rich and erythrocyte-rich thrombosis. Argatroban dose-dependently prevents thrombus formation with an estimated ED50 of 125 μg/kg in this test. Argatroban produces a dose-dependent increases in the thrombin time with a 511% increase at the highest dose used with only a 73% increase in the APTT at this dose. Argatroban can directly induce phenotype conversion of vascular smooth muscle cells with the resultant up-regulation of SMemb, PAI-1, and beta-actin mRNAs.
Br J Pharmacol. 1994 Dec;113(4):1209-14; Jpn J Pharmacol. 1995 Oct;69(2):143-8.
Purity ≥98%
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