生物活性 靶点 体外研究 体内研究
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ChemicalBook  CAS数据库列表  PB28DIHYDROCHLORIDE

PB28DIHYDROCHLORIDE

生物活性 靶点 体外研究 体内研究
PB28DIHYDROCHLORIDE,172906-90-0,结构式
PB28DIHYDROCHLORIDE
  • CAS号:172906-90-0
  • 英文名:PB28dihydrochloride
  • 中文名:PB28DIHYDROCHLORIDE
  • CBNumber:CB91074562
  • 分子式:C24H38N2O
  • 分子量:370.57
  • MOL File:172906-90-0.mol
PB28DIHYDROCHLORIDE化学性质
  • 沸点 :501.4±50.0 °C(Predicted)
  • 密度 :1.032±0.06 g/cm3(Predicted)
  • 储存条件 :Desiccate at +4°C
  • 溶解度 :H2O: ~10mg/mL at 60°C
  • 酸度系数(pKa) :8.32±0.70(Predicted)
  • 形态 :solid
  • 颜色 :white
  • 水溶解性 :H2O: ~10mg/mL at60°C
安全信息
  • 危险品标志 :Xi
  • 危险类别码 :36/37/38
  • 安全说明 :26-36
  • WGK Germany :3

PB28DIHYDROCHLORIDE性质、用途与生产工艺

  • 生物活性 PB28 是一种环己基哌嗪衍生物，是一种 Ki 值为 0.68 nM 的高亲和力和选择性 sigma 2 (σ2) 受体激动剂。PB28 也是一种 σ1 受体拮抗剂，Ki 为 0.38 nM，对其他受体的亲和力较小。PB28 抑制豚鼠膀胱和回肠中的电诱发抽搐，其 EC50 值分别为 2.62 μM 和 3.96 μM。PB28 可以调节 SARS-CoV-2-人之间的蛋白质与蛋白质的相互作用。PB28 可诱导非 caspase 依赖性的细胞凋亡 (apoptosis)，并具有抗肿瘤活性。
  • 靶点

    Ki: 0.68 nM (σ2 receptor); 0.38 nM (σ1 receptor)

  • 体外研究

    PB28 (15-25 nM; 24-48 hours; MCF7 and MCF7 ADR cells) treatment shows an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that are time and concentration independent.
    PB28 has a higher σ2 receptor affinity expressed as K i (0.28 nM and 0.17 nM in MCF7 and MCF7 ADR cells, respectively) than σ1 receptor affinity (13.0 nMand 10.0 nM, respectively).
    PB28 inhibits cell growth of MCF7 and MCF7 ADR cells with IC 50 s of 25 nM and 15 nM, respectively after 2-day treatment.
    PB28 induces apoptosis through a caspase-independent pathway.
    PB28 also reduces P-gp expression in a concentration- and time-dependent manner (approximately 60% in MCF7 and 90% in MCF7 ADR).
    PB28 displays antiproliferative and cytotoxic effects in both C6 rat glioma and SK-N-SH human neuroblastoma cell lines.

    Cell Cycle Analysis

    Cell Line: MCF7 and MCF7 ADR cells
    Concentration: 25 nM and 15 nM
    Incubation Time: 24 hours, 48 hours
    Result: Showed an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that were time and concentration independent.
  • 体内研究

    PB28 (10.7 mg/mL; intraperitoneal injection; daily; for two weeks; C57BL/6 female mice) treatment inhibits tumor growth in Panc02 tumor burden mice. PB28 also conferres a survival advantage for mice.

    Animal Model: C57BL/6 female mice (10 weeks old) injected with Panc02 cells
    Dosage: 10.7 mg/mL
    Administration: Intraperitoneal injection; daily; for two weeks
    Result: Inhibited tumor growth in Panc02 tumor burden mice.
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