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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Diglyceride Acyltransferase (DGAT)-PF-06427878
PF-06427878

Chemical Structure : PF-06427878

CAS No.: 1809064-23-0

PF-06427878 (PF06427878)

货号: PC-73119Not For Human Use, Lab Use Only.

PF-06427878 is a potent, selective, oral DGAT2 inhibitor with IC50 of 99/202 nM for human/rat DGAT2, >470-fold selectivity over DGAT1 and MGAT1/2/3.

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

    生物&药学活性

    PF-06427878 is a potent, selective, oral DGAT2 inhibitor with IC50 of 99/202 nM for human/rat DGAT2, >470-fold selectivity over DGAT1 and MGAT1/2/3.
    PF-06427878 inhibits DGAT2-dependent triglyceride (TG) synthesis in primary human hepatocytes with IC50 of 11.6 nM.
    PF-06427878 reduces hepatic and circulating plasma TG levels as well as lipogenic gene expression in rats maintained on a Western-type diet (0.3-30 mg/kg bid. po.).
    PF-06427878 significantly improves steatosis and hepatocellular ballooning with a decrease in lobular inflammation in a murine nonalcoholic steatohepatitis (NASH) model (2 or 20 mg/kg bid. po.).

    物理化学性质&存储条件

    分子量 476.533
    分子式 C26H28N4O5
    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

    (R)-3-((2-(3-(2-ethoxyphenoxy)piperidin-1-yl)pyrimidine-5-carboxamido)methyl)benzoic acid

    参考文献

    1. Amin NB, et al. Sci Transl Med. 2019 Nov 27;11(520). pii: eaav9701. doi: 10.1126/scitranslmed.aav9701.

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