生物活性 靶点 体外研究 体内研究
ChemicalBook  CAS数据库列表  AR-R17779 HYDROCHLORIDE

AR-R17779 HYDROCHLORIDE

AR-R17779 HYDROCHLORIDE,178419-42-6,结构式
AR-R17779 HYDROCHLORIDE
  • CAS号:178419-42-6
  • 英文名:AR-R 17779 hydrochloride
  • 中文名:AR-R17779 HYDROCHLORIDE
  • CBNumber:CB63037151
  • 分子式:C9H15ClN2O2
  • 分子量:218.68
  • MOL File:178419-42-6.mol
AR-R17779 HYDROCHLORIDE化学性质
  • 储存条件 :-20°C
  • 溶解度 :<10.93mg/ml in DMSO; <21.87mg/ml in H2O
  • 形态 :powder
  • 颜色 :white to beige
  • 旋光性 (optical activity) :[α]/D -59 to -69°, c = 1.0 in methanol

AR-R17779 HYDROCHLORIDE性质、用途与生产工艺

  • 生物活性 AR-R17779 hydrochloride 是一种有效和选择性的 nAChR 全激动剂,对 α7 和 α4β2 亚型的 Ki 直分别为 92 和 16000 nM。AR-R17779 hydrochloride 可以改善大鼠的学习和记忆能力。AR-R17779 hydrochloride 也具有抗焦虑活性。AR-R17779 hydrochloride 可通过激活抗炎胆碱能(迷走神经)途径减轻炎症。
  • 靶点

    IC50: 92 nM (α7-nAChR)

  • 体外研究

    AR-R17779 is 5-fold more potent and 35000-fold more selective than (-)-nicotine for the α7 nicotinic receptor.
    AR-R17779 (200 nM; 24 h) inhibits the LPS-induced TNF production in macrophages.

  • 体内研究

    AR-R17779 (1-5 mg/kg; i.p. twice a day for 7 d) ameliorates arthritis, reduces synovial inflammation, delays onset of disease and protects against joint destruction.
    AR-R17779 (1-10 mg/kg; s.c. for 3 weeks) improves learning in two radial-arm maze tasks and reverses working memory impairment caused by fimbria-fornix sections in rats.

    Animal Model: Male DBA/1 mice (8-10 weeks) were subjected to unilateral cervical vagotomy or sham surgery, after which arthritis was induced with type II collagen
    Dosage: 1, 2.5, 5 mg/kg
    Administration: I.p. twice daily from day 20 until day 26
    Result: Ameliorated arthritis and delayed onset of disease.
    Reduced erosive disease, cartilage degradation and synovial inflammation.
    Reduced TNFα levels in plasma and synovial tissue.
AR-R17779 HYDROCHLORIDE上下游产品信息
上游原料
下游产品
AR-R17779 HYDROCHLORIDE生产厂家
  • 公司名称:MedBio脉铂医药
  • 联系电话:021-69568360 18916172912
  • 电子邮件:order@med-bio.cn
  • 国家:中国
  • 产品数:8141
  • 优势度:58
  • 公司名称:TargetMol中国(陶术生物)
  • 联系电话: 4008200310
  • 电子邮件:marketing@tsbiochem.com
  • 国家:中国
  • 产品数:24647
  • 优势度:58