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S85172

Preladenant

源叶(MedMol) 99%
  • 英文名:
  • Preladenant
  • 别名:
  • CAS号:
  • 377727-87-2
  • 分子式:
  • C25H29N9O3
  • 分子量:
  • 503.56
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S85172-5mg 99% ¥410.00元 10 - - - EA 加入购物车
源叶(MedMol) S85172-10mg 99% ¥650.00元 9 - - - EA 加入购物车
源叶(MedMol) S85172-50mg 99% ¥2050.00元 2 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.
  • 靶点: Ki: 1.1 nM (Adenosine A2A receptor);AdenosineReceptor
  • 体内研究:
    Preladenant (1 mg/kg) inhibits L-Dopa-induced behavioral sensitization after repeated daily administration, which suggests a reduced risk of the development of dyskinesias. Preladenant exhibits antidepressant-like profiles in models of behavioral despair, namely the mouse tail suspension test and the mouse and rat forced swim test. Preladenant produces a dose-dependent reduction in parkinsonian scores at doses of 1 mg/kg (min score: 9.0) and 3 mg/kg (min score: 6.5). A subthreshold dose of Preladenant reduces minimum and mean parkinsonian scores in animals treated with 3 mg kg of L-Dopa to 5.25 and 6.88 respectively. A Wilcoxin test is used to compare individual treatments against vehicle. Preladenant (3 mg/kg), L-Dopa (3, 6, and 12 mg/kg), and the combination of Preladenant and L-Dopa (1 or 3 mg/kg+3 mg/kg) are all significantly improved on the minimum parkinsonian score. In addition, both the 12 mg/kg L-Dopa and L-Dopa+Preladenant groups are significantly improved on both minimum and mean parkinsonian scores relative to the 3 mg/kg L-Dopa group
  • 参考文献:
    1. Hodgson RA, et al. Characterization of the potent and highly selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] in rodent 2. Hodgson RA, et al. Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders. Exp Neurol. 2010 Oct;225(2):384-90.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.986 ml 9.929 ml 19.859 ml
    5 mM 0.397 ml 1.986 ml 3.972 ml
    10 mM 0.199 ml 0.993 ml 1.986 ml
    50 mM 0.04 ml 0.199 ml 0.397 ml
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