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    Argatroban (MD805; MCI9038; Argipidine)
    Argatroban (MD805; MCI9038; Argipidine)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1851
    CAS #: 74863-84-6Purity ≥98%

    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);                           

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    Molecular Weight (MW)508.63 
    FormulaC23H36N6O5S 
    CAS No.74863-84-6 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 9 mg/mL (17.7 mM)
    Water: <1 mg/mL
    Ethanol: 6 mg/mL (11.8 mM)
    Other info

    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 

    SynonymsMD-805; MD 805; MCI-9038;  MCI9038; MCI9038; MD805; DK-7419; DK 7419; DK7419; GN1600; GN-1600; GN 1600; MMTQAP; MPQA; Novastan; OM 805; Slonnon; Argipidine.


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    In Vitro

    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.

    In VivoArgatroban inhibits the formation of microthrombi up to 3 hours after middle cerebral artery (MCA) occlusion; beyond 3 hours, it is ineffective. Argatroban also significantly reduces the size of ischemic cerebral lesions at 6 hours after MCA occlusion. Argatroban (0.3 mg/h/rat) significantly decreases the number of microthrombi 1 day after distal middle cerebral artery (dMCA) occlusion in the rat distal middle cerebral artery occlusion model. Argatroban (0.1 and 0.3 mg/h/rat) significantly reverses a decrease in regional cerebral blood flow (rCBF) 1 day after distal middle cerebral artery (dMCA) occlusion. Argatroban (0.3 mg/h/rat) also significantly reduces the size of the cerebral infarction. 
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    References

    Br J Pharmacol. 1994 Dec;113(4):1209-14; Jpn J Pharmacol. 1995 Oct;69(2):143-8. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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