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BI 665915

Chemical Structure : BI 665915

CAS No.: 1360550-04-4

BI 665915 (BI665915;BI-665915)

Catalog No.: PC-35038Not For Human Use, Lab Use Only.

BI 665915 is a highly potent, selective, orally active 5-lipoxygenase-activating protein (FLAP) inhibitor with binding IC50 of 1.7 nM.

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    Biological Activity

    BI 665915 is a highly potent, selective, orally active 5-lipoxygenase-activating protein (FLAP) inhibitor with binding IC50 of 1.7 nM.
    BI 665915 displays no activity against other enzymes and receptors in the leukotriene pathway such as 5-LO, COX-1 and -2, phospholipase A2, LTA4 hydrolase, BLT1, and BLT2 (IC50s>10 uM).
    BI 665915 shows functional inhibition of LTB4 production in human whole blood (IC50=45 nM).
    BI 665915 demonstrates a dose-dependent DMPK relationship and inhibition of LTB4 production in vivo.

    Physicochemical Properties

    M.Wt 458.526
    Formula C24H26N8O2
    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

    2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide

    References

    1. Takahashi H, et al. J Med Chem. 2015 Feb 26;58(4):1669-90.

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