生物活性 靶点 体外研究 体内研究 纳曲吲哚盐酸盐 试剂级价格
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纳曲吲哚盐酸盐

纳曲吲哚盐酸盐,111469-81-9,结构式
纳曲吲哚盐酸盐
  • CAS号:111469-81-9
  • 英文名:NALTRINDOLE HYDROCHLORIDE
  • 中文名:纳曲吲哚盐酸盐
  • CBNumber:CB3276996
  • 分子式:C26H27ClN2O3
  • 分子量:450.96
  • MOL File:111469-81-9.mol
纳曲吲哚盐酸盐化学性质
  • 储存条件 :−20°C
  • 溶解度 :methanol: 4.5 mg/mL
  • 形态 :solid
  • 颜色 :off-white
安全信息
  • WGK Germany :3

纳曲吲哚盐酸盐性质、用途与生产工艺

  • 生物活性 Naltrindole hydrochloride是高效,选择性的非多肽类 δ opioid 受体拮抗剂,Ki值为0.02 nM。
  • 靶点

    Ki: 0.02 nM (δ opioid), 64 nM (μ opioid), 66 nM (κ opioid)

  • 体外研究

    Opioid drugs exert a wide spectrum of physiological and behavioral effects. These effects are mediated via membrane-bound receptors, of which the best characterized are the kappa, delta, and mu receptors. Naltrindole inhibits the proliferation of cultured human U266 MM cells in a time- and dose-dependent manner with an EC 50 of 16 μM. Treatment of U266 cells with naltrindole significantly decreases the level of the active, phosphorylated form of the kinases, extracellular signal-regulated kinase and Akt, which may be related to its antiproliferative activity. Naltrindole inhibits growth and induces apoptosis in the three characteristic SCLC cell lines, NCI-H69, NCI-H345, and NCI-H510. Naltrindole treatment reduces constitutive phosphorylation of Akt/PKB on serine 473 and threonine 308 in cells and also its downstream effectors glycogen synthase kinase-3β and the Forkhead transcription factors AFX and FKHR.

  • 体内研究

    Naltrindole significantly decreases tumor cell volumes in human MM cell xenografts in severe combined immunodeficient mice. In mice, naltrindole at 20 mg/kg s.c. antagonizes the δ-selective agonist effect of [D- Ser, Leu, Thr]enkephalin (DSLET) without blocking the antinociceptive effect of morphine or U50488H. Naltrindole is the only highly selective δ antagonist that is active upon peripheral administration. Acute naltrindole induces significant decreases in external and total ambulation (horizontal activity) and rearing behaviour (vertical activity), as well as a significant increase in grooming frequency. In animals chronically treated with naltrindole there is an increase in total ambulation one day after the discontinuation of the treatment.

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纳曲吲哚盐酸盐 试剂级价格
  • 更新日期:2022/09/18
  • 产品编号:HY-101177
  • 产品名称:纳曲吲哚盐酸盐 Naltrindole hydrochloride
  • CAS编号:111469-81-9
  • 包装:5mg
  • 价格:990元
  • 更新日期:2022/09/18
  • 产品编号:HY-101177
  • 产品名称:纳曲吲哚盐酸盐 Naltrindole hydrochloride
  • CAS编号:111469-81-9
  • 包装:10mM * 1mLin DMSO
  • 价格:1089元
纳曲吲哚盐酸盐生产厂家
  • 公司名称:Labinova AB
  • 联系电话:--
  • 电子邮件:info@labinova.se
  • 国家:欧洲
  • 产品数:281
  • 优势度:64
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