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首页-小分子抑制剂&激动剂-GPCR-GPR119-BMS-903452
BMS-903452

Chemical Structure : BMS-903452

CAS No.: 1339944-47-6

BMS-903452 (BMS 903452)

货号: PC-20435Not For Human Use, Lab Use Only.

BMS-903452 (BMS 903452) is a potent and selective GPR119 agonist with EC50 of 14 nM.

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

    生物&药学活性

    BMS-903452 (BMS 903452) is a potent and selective GPR119 agonist with EC50 of 14 nM.
    BMS-903452 exhibits an excellent profile in our vitro safety assays, no significant inhibition (IC50 > 40 μM) at nine different cytochrome P450 enzymes, does not activate PXR (EC50>50 μM), and exhibits no toxicity in a hepatic (HEPG2) cell line.
    BMS-903452 displays high selectivity against a panel of 95 GPCRs and enzymes in a broad receptor screening panel.
    BMS-903452 significantly increased active GLP-1 levels in cannulated Sprague-Dawley rat model.
    BMS-903452 exhibited synergistic effect when combined with DPPIV inhibitor.
    BMS-903452 is efficacious in both acute and chronic in vivo rodent models of diabetes.

    物理化学性质&存储条件

    分子量 513.37
    分子式 C21H19Cl2FN4O4S
    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

    5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one

    参考文献

    1. Wacker DA, et al. J Med Chem. 2014 Sep 25;57(18):7499-508.

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