A thrombin inhibitor
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Labeled Version(s)
25757Argatroban-d3 (hydrochloride)
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Argatroban

Item No. 19639

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 3 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): 0.1 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $41

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    10 mg

    $69

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    25 mg

    $157

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    50 mg

    $293

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    Product Description

    Argatroban is a reversible inhibitor of thrombin (IC50s = 0.01 and 0.09 µM for the free and clot-bound forms, respectively).1 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.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Park, H.D., Lee, S.H., Kim, T.H., et al. Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug. Bioorg. Med. Chem. Lett. 23(17), 4779-4784 (2013).

    2. Kato, Y., Kita, Y., Hirasawa-Taniyama, Y., et al. Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig. Eur. J. Pharmacol. 473(2-3), 163-169 (2003).