
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)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥510 | 有现货 |
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5MG | ¥786 | 有现货 |
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10MG | ¥1442 | 有现货 |
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25MG | ¥2697 | 有现货 |
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50MG | ¥4496 | 有现货 |
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100MG | ¥6464 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称Almorexant
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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
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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。
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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.
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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.
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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.
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同义词ACT-078573 | ACT 078573 | ACT078573
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通路GPCR/G Protein
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靶点Orexin Receptor
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受体OX1|OX2
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研究领域Neurological Disease
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适应症Sleep Disorder
化学信息
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CAS Number871224-64-5
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分子量512.5632
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分子式C29H31F3N2O3
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESCNC(=O)[C@H](N1CCc2cc(OC)c(OC)cc2[C@@H]1CCc3ccc(cc3)C(F)(F)F)c4ccccc4
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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
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储存条件(-20℃)
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运输条件With Ice Pack
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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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