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Almorexant

CAS No. 871224-64-5

Almorexant ( ACT-078573 | ACT 078573 | ACT078573 )

产品货号. M16329 CAS No. 871224-64-5

一种双重 Orexin 受体 OX1/OX2 拮抗剂,hOX1/hOX2 的 Ki 值分别为 1.3/0.17 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥510 有现货
5MG ¥786 有现货
10MG ¥1442 有现货
25MG ¥2697 有现货
50MG ¥4496 有现货
100MG ¥6464 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Almorexant
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    一种双重 Orexin 受体 OX1/OX2 拮抗剂,hOX1/hOX2 的 Ki 值分别为 1.3/0.17 nM。
  • 产品描述
    A dual Orexin receptor OX1/OX2 antagonist with Ki of 1.3/0.17 nM for hOX1/hOX2 respectively; selectively inhibits the functional consequences of OX1 and OX2 receptor activation, such as intracellular Ca2+ mobilization.Sleep Disorder Phase 3 Discontinued(In Vitro):Almorexant (1 μM) promotes tyrosine phosphorylation of SHP2/OX1R complex.Almorexant (1 μM) inhibits the cellular growth of AsPC-1 cells.(In Vivo):Almorexant (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors.Almorexant (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning.Almorexant (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy18 or deficits in next-day performance.
  • 体外实验
    Almorexant (1 μM) promotes tyrosine phosphorylation of SHP2/OX1R complex.Almorexant (1 μM) inhibits the cellular growth of AsPC-1 cells.
  • 体内实验
    Almorexant (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors.Almorexant (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning. Almorexant (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy18 or deficits in next-day performance. Animal Model:Mice xenografted with AsPC-1 cells Dosage:1.8 μmol/kg, 100 μL Administration:IP, daily, starting at day 0 or day 38 Result:Resulted in a significant decrease in tumor volume when treatment starting at day 0. Started after AsPC-1 tumors were developed (day 38), rapidly and strongly reduced the volume of established tumors.Animal Model:Long-Evans rats (24, male, 16-18 weeks of age) Dosage:300 mg/kg Administration:PO, once Result:Successfully learned the spatial task, established spatial memory.Animal Model:Male C57BL/6 mice (Orexin/ataxin-3 transgenic (TG) mice and WT mice, 32 ± 0.9 g, age 15 ± 0.5 week)Dosage:30, 100, 300 mg/kg (3, 10, and 30 mg/mL; 10 mL/kg) Administration:IP, once every 3 days Result:Exacerbated cataplexy in TG mice and increased nonrapid eye movement (NREM) sleep with heightened sleep/wake fragmentation in both genotypes during the 12-h dark period after dosing. Showed greater hypnotic potency in WT mice than in TG mice.
  • 同义词
    ACT-078573 | ACT 078573 | ACT078573
  • 通路
    GPCR/G Protein
  • 靶点
    Orexin Receptor
  • 受体
    OX1|OX2
  • 研究领域
    Neurological Disease
  • 适应症
    Sleep Disorder

化学信息

  • CAS Number
    871224-64-5
  • 分子量
    512.5632
  • 分子式
    C29H31F3N2O3
  • 纯度
    >98% (HPLC)
  • 溶解度
    10 mM in DMSO
  • SMILES
    CNC(=O)[C@H](N1CCc2cc(OC)c(OC)cc2[C@@H]1CCc3ccc(cc3)C(F)(F)F)c4ccccc4
  • 化学全称
    2(1H)-Isoquinolineacetamide, 3,4-dihydro-6,7-dimethoxy-N-methyl-α-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-, (αR,1S)-

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Malherbe P, et al. Mol Pharmacol. 2009 Sep;76(3):618-31. 2. Malherbe P, et al. Mol Pharmacol. 2010 Jul;78(1):81-93. 3. Li A, et al. J Physiol. 2010 Aug 1;588(Pt 15):2935-44.
产品手册
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