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GE1111

Chemical Structure : GE1111

CAS No.: 2883669-12-1

GE1111 (GE-1111)

Catalog No.: PC-49486Not For Human Use, Lab Use Only.

GE1111 is a novel potent small molecule Mas-related G protein-coupled receptor X2 (MRGPRX2) antagonist, significantly inhibits mast cells degranulation and MRGPRX2 activation with IC50 of 5 uM.

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    Biological Activity

    GE1111 is a novel potent small molecule Mas-related G protein-coupled receptor X2 (MRGPRX2) antagonist, significantly inhibits mast cells degranulation and MRGPRX2 activation with IC50 of 5 uM.
    GE1111 inhibited not only the early phase of mast cell activation but also the late phase, associated with chemokine and prostaglandin release, inhibited downstream PLC-γ, ERK1/2 and Akt signalling pathway.
    GE1111 attenuated C48/80-induced mouse peritoneal mast cells degranulation, paw oedema and tissue extravasation in allergic mice models.

    Physicochemical Properties

    M.Wt 466.49
    Formula C28H22N2O5
    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

    methyl 3-(2-formyl-9-hydroxy-1-methyl-1H-phenalen-5-yl)-7-ureido-2-naphthoate

    References

    1. Kumar M, et al. J Allergy Clin Immunol. 2022 Dec 26:S0091-6749(22)02551-9.

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