Argatroban

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 (Kis = 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.Formal Name: (2R,4R)-1-[(2S)-5-[(aminoiminomethyl)amino]-1-oxo-2-[[(1,2,3,4-tetrahydro-3-methyl-8-quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2-piperidinecarboxylic acid. CAS Number: 74863-84-6. Synonyms: MCI-9038. Molecular Formula: C23H36N6O5S. Formula Weight: 508.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 3 mg/ml, Ethanol: 1 mg/ml, PBS (pH 7.2): 0.1 mg/ml. lambdamax: 212, 259, 331 nm. SMILES: CC1CC2=C(C(S(N[C@@H](CCCNC(N)=N)C(N3[C@@H](C(O)=O)C[C@H](C)CC3)=O)(=O)=O)=CC=C2)NC1. InChi Code: InChI=1S/C23H36N6O5S/c1-14-8-10-29(18(12-14)22(31)32)21(30)17(6-4-9-26-23(24)25)28-35(33,34)19-7-3-5-16-11-15(2)13-27-20(16)19/h3,5,7,14-15,17-18,27-28H,4,6,8-13H2,1-2H3,(H,31,32)(H4,24,25,26)/t14-,15?,17+,18-/m1/s1. InChi Key: KXNPVXPOPUZYGB-IOVMHBDKSA-N.