A plasma kallikrein inhibitor
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Sebetralstat

Item No. 45043

Product Insert (PDF)
Technical Information
Formal Name
N-[(3-fluoro-4-methoxy-2-pyridinyl)methyl]-3-(methoxymethyl)-1-[[4-[(2-oxo-1(2H)-pyridinyl)methyl]phenyl]methyl]-1H-pyrazole-4-carboxamide
CAS Number
1933514-13-6
Synonyms
  • KVD900
Molecular Formula
C26H26FN5O4
Formula Weight
Purity
≥95%
A solid
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1C=CC=CN1CC2=CC=C(CN3N=C(COC)C(C(NCC4=NC=CC(OC)=C4F)=O)=C3)C=C2
InChi Code
InChI=1S/C26H26FN5O4/c1-35-17-22-20(26(34)29-13-21-25(27)23(36-2)10-11-28-21)16-32(30-22)15-19-8-6-18(7-9-19)14-31-12-4-3-5-24(31)33/h3-12,16H,13-15,17H2,1-2H3,(H,29,34)
InChi Key
KGMPDQIYDKKXRD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Sebetralstat is an inhibitor of plasma kallikrein (IC50 = 6 nM).1 It is selective for plasma kallikrein over a panel of 14 additional proteases (IC50s = >10 µM for all). Sebetralstat (50-1,000 nM) inhibits dextran sulfate-induced cleavage of kininogen-1 in isolated human plasma. Formulations containing sebetralstat have been used in the treatment of acute hereditary angioedema (HAE).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Duckworth, E.J., Murugesan, N., Li, L., et alPharmacological suppression of the kallikrein kinin system with KVD900: An orally available plasma kallikrein inhibitor for the on-demand treatment of hereditary angioedema. Clin. Exp. Allergy 52(9), 1059-1070 (2022).