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GSK2973980A

Chemical Structure : GSK2973980A

CAS No.: 1414797-35-5

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GSK2973980A (GSK 2973980A)

Catalog No.: PC-62635Not For Human Use, Lab Use Only.

GSK2973980A is a potent and selective DGAT1 inhibitor with IC50 of 3 nM, exhibits >2,900-fold selectivity over human DGAT2, ACAT1 and ACAT2 (IC50>10 uM).

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

    Biological Activity

    GSK2973980A is a potent and selective DGAT1 inhibitor with IC50 of 3 nM, exhibits >2,900-fold selectivity over human DGAT2, ACAT1 and ACAT2 (IC50>10 uM).
    GSK2973980A exhibits IC50 value of 77 nM in the cell-based C2C12 assay, also has excellent cardiac ion channel profile with IC50 of >10 uM in the hERG, Nav1.5 and Cav1.2。
    GSK2973980A demonstrates excellent DMPK profiles and in vivo efficacy in a postprandial lipid excursion model in mice.

    Physicochemical Properties

    M.Wt 534.443
    Formula C25H19F5N4O4
    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

    (S)-2-(6-(5-(3-(3,4-difluorophenyl)ureido)pyrazin-2-yl)-1-oxo-2-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)acetic acid

    References

    1. Cheung M, et al. ACS Med Chem Lett. 2018 Jan 16;9(2):103-108.

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