An internal standard for the quantification of argatroban
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Unlabeled Version(s)
19639Argatroban
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Argatroban-d3 (hydrochloride)

Item No. 25757

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-d3-8-quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2-piperidinecarboxylic acid, monohydrochloride
CAS Number
1356847-56-7
Molecular Formula
C23H33D3N6O5S • HCl
Formula Weight
548.1
Purity
≥99% deuterated forms (d1-d3)
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: SolubleDMSO: SolubleMethanol: Soluble
SMILES
O=S(C1=CC=CC2=C1NCC(C([2H])([2H])[2H])C2)(N[C@@H](CCCNC(N)=N)C(N3[C@@H](C(O)=O)C[C@H](C)CC3)=O)=O
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/i2D3
InChi Key
KXNPVXPOPUZYGB-HKEDOSAWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $329

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    5 mg

    $1,474

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    Product Description

    Argatroban-d3 is intended for use as an internal standard for the quantification of argatroban (Item No. 19639) 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).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).