Almorexant hydrochloride

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.

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Animal Model:Mice xenografted with AsPC-1 cellsDosage:1.8 μmol/kg, 100 μLAdministration: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 daysResult: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 hydrochloride | ACT 078573 hydrochloride | ACT078573 hydrochloride

GPCR/G Protein

Orexin Receptor

OX1|OX2

Neurological Disease

Sleep Disorder

913358-93-7

549.0242

C29H32ClF3N2O3

>98% (HPLC)

DMSO: ≥ 46 mg/mL

O=C([C@H](N1CCC2=C([C@@H]1CCC3=CC=C(C=C3)C(F)(F)F)C=C(C(OC)=C2)OC)C4=CC=CC=C4)NC.[H]Cl

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

(-20℃)

With Ice Pack

≥ 2 years