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EXEL-0346

Chemical Structure : EXEL-0346

CAS No.: 1239893-96-9

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EXEL-0346 (EXEL0346)

Catalog No.: PC-61427Not For Human Use, Lab Use Only.

EXEL-0346 (EXEL0346) is a novel potent, orally active Glucosylceramide synthase (GCS) inhibitor with IC50 of 2 nM.

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

    Biological Activity

    EXEL-0346 (EXEL0346) is a novel potent, orally active Glucosylceramide synthase (GCS) inhibitor with IC50 of 2 nM.
    EXEL-0346 decreases glucosylceramide synthesis and ganglioside GM1 synthesis in A549 cells with IC50 of 15 nM.
    EXEL-0346 robustly improves glucose tolerance in diet induced obese mice and ZDF rats, decreases plasma triglycerides and reduces hepatic fat deposition.
    EXEL-0346 exhibits excellent oral bioavailability coupled with the long half-life.

    Physicochemical Properties

    M.Wt 580.446
    Formula C27H29BrF3N3O3
    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

    N-[(1S)-2-(3-Amino-8-azabicyclo[3.2.1]oct-8-yl)-1-[(4-bromophenyl)methyl]-2-oxoethyl]-1-[4-[(trifluoromethyl)oxy]-phenyl]cyclopropanecarboxamide

    References

    1. Richards S, et al. J Med Chem. 2012 May 10;55(9):4322-35.

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