Almorexant

Research use only, not for human use.

A dual Orexin receptor OX1/OX2 antagonist with Ki of 1.3/0.17 nM for hOX1/hOX2 respectively.

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.

Almorexant (1 μM) promotes tyrosine phosphorylation of SHP2/OX1R complex.Almorexant (1 μM) inhibits the cellular growth of AsPC-1 cells.

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.

ACT-078573 | ACT 078573 | ACT078573

GPCR/G Protein

Orexin Receptor

OX1|OX2

Neurological Disease

Sleep Disorder

871224-64-5

512.5632

C29H31F3N2O3

>98% (HPLC)

10 mM in DMSO

CNC(=O)[C@H](N1CCc2cc(OC)c(OC)cc2[C@@H]1CCc3ccc(cc3)C(F)(F)F)c4ccccc4

2(1H)-Isoquinolineacetamide, 3,4-dihydro-6,7-dimethoxy-N-methyl-α-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-, (αR,1S)-

(-20℃)

With Ice Pack

≥ 2 years