生物活性 靶点 体外研究 体内研究 丙酸倍氯松二溴酸盐 试剂级价格
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ChemicalBook  CAS数据库列表  丙酸倍氯松二溴酸盐

丙酸倍氯松二溴酸盐

生物活性 靶点 体外研究 体内研究 丙酸倍氯松二溴酸盐 试剂级价格
丙酸倍氯松二溴酸盐,145231-35-2,结构式
丙酸倍氯松二溴酸盐
  • CAS号:145231-35-2
  • 英文名:N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA
  • 中文名:丙酸倍氯松二溴酸盐
  • CBNumber:CB42463700
  • 分子式:C14H17ClN4S.2BrH
  • 分子量:470.659
  • MOL File:145231-35-2.mol
丙酸倍氯松二溴酸盐化学性质
  • 熔点 :205°C(lit.)
  • 储存条件 :Store at -20°C
  • 溶解度 :DMSO: 30 mg/ml; Ethanol: 2.5 mg/ml; Water: 20 mg/ml
  • 形态 :powder to crystal
  • 颜色 :White to Gray to Red
  • 水溶解性 :Soluble to 100 mM in water
安全信息
  • 海关编码 :2933.29.4300

丙酸倍氯松二溴酸盐性质、用途与生产工艺

  • 生物活性 Clobenpropit dihydrobromide 是一种有效的组胺 H3R 拮抗剂/反向激动剂，对组胺 H3LR 的 pEC 50 为 8.07。Clobenpropit dihydrobromide 对组胺 H4 受体起部分激动剂的作用，Ki 为 13 nM。Clobenpropit dihydrobromide 还与 5-HT3 受体 (Ki 为 7.4 nM) 和 α2A/α2C 肾上腺素受体 (Ki 为 17.4/7.8 nM) 结合。Clobenpropit dihydrobromide 促进凋亡 (apoptosis)。
  • 靶点

    Human H3LR

    9.44 (pKi)

    Rat H3LR

    9.75 (pKi)

    H 4 receptor

    13 nM (Ki)

    H 2 Receptor

    5.6 (pKi)

  • 体外研究

    Clobenpropit binds to human H3LR and rat H3LR with pK i s of 9.44±0.04 and 9.75±0.01. Clobenpropit exhibits low affinity for histamine H1R or H2R (pK i s of 5.2 and 5.6, respectively).
    Clobenpropit inhibits [ 3 H]-dopamine transport by SH-SY5Y cells in a concentration dependent manner with maximum inhibition 82.7±2.8 % and IC 50 490 nM (pIC 50 6.31±0.11).
    Clobenpropit is a subunit-selective noncompetitive antagonist at recombinant NMDA receptors (IC 50 1 μM for the NR1/NR2B receptor).
    Clobenpropit (50 μM) and Gemcitabine (5 μM) combination therapy significantly increases apoptosis of Panc-1, MiaPCa-2 and AsPC-1 compared with control.

    Apoptosis Analysis

    Cell Line: Pancreatic cancer cells (Panc-1, MiaPaCa-2 and AsPC-1)
    Concentration: 50 μM
    Incubation Time:
    Result: Enhanced apoptotic cell death in combination of Gemcitabine (5 μM).
  • 体内研究

    The combination treatment of Clobenpropit (every other day intraperitoneal injection at 20 μM per kilogram for 40 d) and Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d) shows significant tumor growth inhibition.

    Animal Model: Five-week-old male BALB/c nude mice with Panc-1 xenograft
    Dosage: 20 μM per kilogram
    Administration: Intraperitoneal injection; every other day for 40 days. Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d)
    Result: The combination treatment showed significant tumor growth inhibition compared with other treatment groups (control 501±92 mg, Gemcitabine 294±46 mg, Clobenpropit 444±167 mg, and combination 154±54 mg).
丙酸倍氯松二溴酸盐上下游产品信息
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丙酸倍氯松二溴酸盐 试剂级价格
  • 更新日期：2024/11/08
  • 产品编号：C3446
  • 产品名称：氯苯丙替二氢溴酸盐 Clobenpropit Dihydrobromide
  • CAS编号：145231-35-2
  • 包装：25mg
  • 价格：905元
丙酸倍氯松二溴酸盐生产厂家
  • 公司名称：TCI Europe
  • 联系电话：320-37350700
  • 电子邮件：sales@tcieurope.eu
  • 国家：欧洲
  • 产品数：23671
  • 优势度：75
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