An inhibitor of uPA
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ZK 824859

Item No. 37789

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[6-[[3′-(aminomethyl)[1,1′-biphenyl]-3-yl]oxy]-3,5-difluoro-2-pyridinyl]oxy]-butanoic acid
CAS Number
2254001-81-3
Molecular Formula
C22H20F2N2O4
Formula Weight
414.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
SMILES
NCC1=CC=CC(C2=CC(OC3=C(F)C=C(F)C(O[C@H](CC)C(O)=O)=N3)=CC=C2)=C1
InChi Code
InChI=1S/C22H20F2N2O4/c1-2-19(22(27)28)30-21-18(24)11-17(23)20(26-21)29-16-8-4-7-15(10-16)14-6-3-5-13(9-14)12-25/h3-11,19H,2,12,25H2,1H3,(H,27,28)/t19-/m1/s1
InChi Key
ZDHMLADHONAIES-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $61

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    10 mg

    $116

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    25 mg

    $273

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    50 mg

    $484

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    Product Description

    ZK 824859 is an inhibitor of urokinase-type plasminogen activator (uPA; IC50s = 79 and 410 nM for the human and mouse proteins, respectively).1 It is selective for human uPA over human tissue-type plasminogen activator (tPA) and plasmin (IC50s = 1,580 and 1,330 nM, respectively) but not selective for mouse uPA over mouse tPA and plasmin (IC50s = 910 and 1,600 nM, respectively). ZK 824859 (25 or 50 mg/kg per day) reduces the incidence of limb weakness and paralysis in mice in a model of experimental autoimmune encephalomyelitis (EAE).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Islam, I., Yuan, S., West, C.W., et al. Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis. Bioorg. Med. Chem. Lett. 28(20), 3372-3375 (2018).