生物活性 靶点 体外研究 体内研究
ChemicalBook  CAS数据库列表  1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride

1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride

1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride,1164469-60-6,结构式
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
  • CAS号:1164469-60-6
  • 英文名:1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
  • 中文名:1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride
  • CBNumber:CB73845715
  • 分子式:C24H29ClN2O3
  • 分子量:428.95166
  • MOL File:1164469-60-6.mol
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride化学性质
  • 储存条件 :Store at -20°C
  • 溶解度 :DMF: 10 mg/mL; DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL; DMSO: 3 mg/mL
  • 形态 :A crystalline solid

1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride性质、用途与生产工艺

  • 生物活性 Naftopidil hydrochloride (KT-611 hydrochloride) 是一种选择性的 alpha1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂,对克隆的人类 α1a、α1b 和 α1d 亚型肾上腺素受体的亲和力 Ki 值分别为 3.7 nM、20 nM、1.2 nM,具有抗增殖作用。Naftopidil hydrochloride 可用于前列腺增生的研究。
  • 靶点

    Alpha-1A adrenergic receptor

    3.7 nM (Ki)

    Alpha-1B adrenergic receptor

    20 nM (Ki)

    Alpha-1D adrenergic receptor

    1.2 nM (Ki)

  • 体外研究

    Naftopidil hydrochloride suppresses human prostate tumor growth by altering interactions between tumor cells and stroma.
    Naftopidil hydrochloride (10 μM for PCa cells, 0.1-10 μM for PrSC; 3 days) shows growth inhibitory effects on PCa cells and PrSC.
    Naftopidil hydrochloride (50 μM for E9 cells, 25 μM for PrSC; 48 hours) increases the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC.

    Cell Proliferation Assay

    Cell Line: PCa cells, PrSC
    Concentration: 10 μM (PCa cells); 0.1 μM, 1 μM, 10 μM (PrSC)
    Incubation Time: 3 days
    Result: Exhibited growth inhibitory effects on PCa cells and PrSC in dose-dependent manners.

    Western Blot Analysis

    Cell Line: PCa cells, PrSC
    Concentration: 50 μM (E9 cells), 25 μM (PrSC)
    Incubation Time: 48 hours
    Result: Increased the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC.
  • 体内研究

    Naftopidil hydrochloride (10 mg/kg; p.o; daily; for 28 days) decreases microvessel density (MVD) in E9+PrSC tumors mice model.

    Animal Model: Male athymic mice(7-8 weeks), with E9+PrSC xenograft
    Dosage: 10 mg/kg
    Administration: Oral administration, daily, for 28 days
    Result: Decreased tumor weights.
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol:hydrochloride上下游产品信息
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