Almorexant

SKU: orb1223792

Description

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.

Key Properties

• CAS Number: 871224-64-5
• MW: 512.5632
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₁F₃N₂O₃
• SMILES: CNC(=O)[C@H](N1CCc2cc(OC)c(OC)cc2[C@@H]1CCc3ccc(cc3)C(F)(F)F)c4ccccc4
• Target: Orexin Receptor
• Solubility: 10 mM in DMSO

Bioactivity

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

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ACT-078573 | ACT 078573 | ACT078573

Quick Database Links

Gene Symbol

Orexin Receptor