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ChemicalBook  CAS数据库列表  N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine

N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine

生物活性 体外研究 体内研究
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine,1438071-12-5,结构式
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
  • CAS号:1438071-12-5
  • 英文名:N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
  • 中文名:N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
  • CBNumber:CB63464337
  • 分子式:C20H18Cl2N2O2S
  • 分子量:421.34
  • MOL File:1438071-12-5.mol
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine化学性质
  • 沸点 :525.0±45.0 °C(Predicted)
  • 密度 :1.363±0.06 g/cm3(Predicted)
  • 溶解度 :Acetonitrile (Slightly), DMSO (Slightly, Heated), Methanol (Slightly, Sonicated)
  • 酸度系数(pKa) :5.23±0.50(Predicted)
  • 形态 :Solid
  • 颜色 :Off-White to Light Beige
  • 稳定性 :Hygroscopic

N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine性质、用途与生产工艺

  • 生物活性 GSK2945 是一类叔胺，是一种高度特异性的 Rev-erbα/REV-ERBα (小鼠/人反向成红细胞病病毒α) 拮抗剂， 其 EC50 值分别为 21.5 μM 和 20.8 μM。GSK2945 可增强胆固醇 7α-羟化酶 (CYP7A1) 水平和胆固醇代谢。
  • 体外研究

    GSK2945 dose-dependently enhances the transcriptional activity of Rev-erbα and a Bmal1 (a target gene of REV-ERBs) luciferase reporter ( EC 50 of 2.05 μM).
    GSK2945 (20 μM; 12 hours and 24 hours; mouse and human primary hepatocytes) treatment increases levels of Cyp7a1/CYP7A1 in mouse and human primary hepatocytes. GSK2945 (20 μM) treatment also increases Lrh-1/LRH-1 (a known hepatic activator of Cyp7a1/CYP7A1) mRNA and protein.

    RT-PCR

    Cell Line: Mouse (male, CD1) and human (male, Caucasian) primary hepatocytes
    Concentration: 20 μM
    Incubation Time: 12 hours and 24 hours
    Result: Led to significant increases in mRNA and protein (at 24-h) expression of Cyp7a1. mRNA and protein (at 24-h) levels of CYP7A1 were increased in human primary hepatocyte. Lrh-1/LRH-1 was upregulated.
  • 体内研究

    GSK2945 (0-10 mg/kg; intraperitoneal injection; twice every day; for 7 days; male C57BL/6 mice) treatment increases hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowers plasma cholesterol in wild-type mice.

    Animal Model: Male C57BL/6 mice (8-10 weeks of age)
    Dosage: 0 mg/kg or 10 mg/kg
    Administration: Intraperitoneal injection; twice every day; for 7 days
    Result: Increased hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice.
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N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine生产厂家
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