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BI1002494

Chemical Structure : BI1002494

CAS No.: 1319738-39-0

BI1002494 (BI 1002494)

Catalog No.: PC-70329Not For Human Use, Lab Use Only.

BI1002494 (BI-1002494) is a novel, potent, and selective spleen tyrosine kinase (SYK) inhibitor with enzyme IC50 of 30 nM, cell IC50 of 7 nM (FcεR1-mediated histamine release in human monocyte-derived mast cells, in the presence of 0.1% albumin).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    BI1002494 (BI-1002494) is a novel, potent, and selective spleen tyrosine kinase (SYK) inhibitor with enzyme IC50 of 30 nM, cell IC50 of 7 nM (FcεR1-mediated histamine release in human monocyte-derived mast cells, in the presence of 0.1% albumin).
    BI1002494 inhibits high-affinity IgE receptor-mediated mast cell and basophil degranulation (IC50=115 nM), 7-fold lower potency for blocking CD69 expression after anti-IgD (BCR) stimulation of peripheral B cells.
    BI1002494 dose-dependently inhibited OVA-induced bronchioalveolar lavage eosinophils in brown Norway rats.

    Physicochemical Properties

    M.Wt 423.469
    Formula C23H25N3O5
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (R)-4-((R)-1-((7-(3,4,5-trimethoxyphenyl)-1,6-naphthyridin-5-yl)oxy)ethyl)pyrrolidin-2-one

    References

    1. Lamb DJ, et al. J Pharmacol Exp Ther. 2016 Jun;357(3):554-61.

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