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BI 135585

Chemical Structure : BI 135585

CAS No.: 1114561-85-1

BI 135585 (BI-135585;BI135585)

Catalog No.: PC-60448Not For Human Use, Lab Use Only.

BI 135585 (BI-135585, BI135585) is a potent, selective, orally active 11β-HSD1 inhibitor with IC50 of 4.3 nM and 53 nM in human adipocytes and primary human adipose tissue, respectively.

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

    Biological Activity

    BI 135585 (BI-135585, BI135585) is a potent, selective, orally active 11β-HSD1 inhibitor with IC50 of 4.3 nM and 53 nM in human adipocytes and primary human adipose tissue, respectively.
    BI 135585 exhibits >1,000-fold selectivity over other hydroxysteroid dehydrogenases.
    BI 135585 inhibits 11β HSD1 activity in adipose tissue, displays desirable pharmacodynamic properties in vivo.

    Physicochemical Properties

    M.Wt 460.574
    Formula C28H32N2O4
    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)-6-(2-hydroxy-2-methylpropyl)-3-((S)-1-(4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl)ethyl)-6-phenyl-1,3-oxazinan-2-one

    References

    1. Hamilton BS, et al. Eur J Pharmacol. 2015 Jan 5;746:50-5.

    2. Freude S, et al. Diabetes Obes Metab. 2016 May;18(5):483-90.

    3. Zhuang L, et al. Bioorg Med Chem. 2017 Jul 15;25(14):3649-3657.

    4. Hamilton BS, et al. Eur J Pharmacol. 2016 Oct 15;789:68-74.

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