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SKI-2852

Chemical Structure : SKI-2852

CAS No.: 1346554-47-9

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SKI-2852 (SKI 2852;SKI2852)

Catalog No.: PC-61137Not For Human Use, Lab Use Only.

SKI-2852 is a highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively.

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

    Biological Activity

    SKI-2852 is a highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively.
    SKI-2852 demonstrates no CYP and PXR liabilities, excellent PK profiles across species, and highly potent and sustainable PD activity.
    SKI-2852 significantly reduces blood glucose and HbA1c levels and improves the lipid profiles in ob/ob mice, synergistically enhances the HbA1c-lowering effect of metformin in vivo.

    Physicochemical Properties

    M.Wt 543.658
    Formula C27H34FN5O4S
    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-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide

    References

    1. Ryu JH, et al. J Med Chem. 2016 Nov 23;59(22):10176-10189.

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