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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-11β-HSD-BI 135585
BI 135585

Chemical Structure : BI 135585

CAS No.: 1114561-85-1

BI 135585 (BI-135585;BI135585)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 460.574
    分子式 C28H32N2O4
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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

    参考文献

    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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