An inhibitor of plasma kallikrein
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PKSI-527

Item No. 23974

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[(2S)-2-[[[trans-4-(aminomethyl)cyclohexyl]carbonyl]amino]-1-oxo-3-phenylpropyl]amino]-benzeneacetic acid, monohydrochloride
CAS Number
128837-71-8
Molecular Formula
C25H31N3O4 • HCl
Formula Weight
474.0
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Water: 10 mM
SMILES
NC[C@@H]1CC[C@@H](C(N[C@@H](CC2=CC=CC=C2)C(NC3=CC=C(CC(O)=O)C=C3)=O)=O)CC1.Cl
InChi Code
InChI=1S/C25H31N3O4.ClH/c26-16-19-6-10-20(11-7-19)24(31)28-22(14-17-4-2-1-3-5-17)25(32)27-21-12-8-18(9-13-21)15-23(29)30;/h1-5,8-9,12-13,19-20,22H,6-7,10-11,14-16,26H2,(H,27,32)(H,28,31)(H,29,30);1H/t19-,20-,22-;/m0./s1
InChi Key
NAXNMKUKSBHHMP-JLBKCEDKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $83

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    25 mg

    $330

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    Product Description

    PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM).1 It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wanaka, K., Okamoto, S., Bohgaki, M., et al. Effect of a highly selective plasma-kallikrein synthetic inhibitor on contact activation relating to kinin generation, coagulation and fibrinolysis. Thromb. Res. 57(6), 889-895 (1990).

    2. Fujimori, Y., Nakamura, T., Shimizu, K., et al. Effects of a highly selective plasma kallikrein inhibitor on collagen-induced arthritis in mice. Agents Actions 39(1-2), 42-48 (1993).