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Almorexant

Cat. No. M3261

All AbMole products are for research use only, cannot be used for human consumption.

Almorexant Structure
Synonym:

ACT-078573

Size Price Availability Quantity
1mg USD 55  USD55 In stock
5mg USD 110  USD110 In stock
10mg USD 175  USD175 In stock
25mg USD 350  USD350 In stock
50mg USD 550  USD550 In stock
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Quality Control & Documentation
Biological Activity

Almorexant (ACT-078573) is a competitive OX1 and OX2 orexin receptor antagonist with IC50 of 13 and 8 nM, respectively. It is rapidly absorbed and distributed and shows no tendency to accumulate with repeated dosing. Preclinical studies in rats and dogs have demonstrated a sleep-promoting effect which resembles physiological sleep; this could be quickly reversed upon sensorimotor stimulation and yet allow resumption of sleep upon its cessation. Almorexant’s (ACT-078573) sleep-promoting effects were confirmed in volunteers and patients with primary insomnia. It dose-dependently increased sleep efficiency and decreased sleep latency and wake time after sleep onset.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Wistar rats.
Formulation Polyethylene glycol (PEG) 400 or 0.25% methylcellulose in water
Dosages ~300 mg/kg
Administration p.o.
Chemical Information
Molecular Weight 512.56
Formula C29H31F3N2O3
CAS Number 871224-64-5
Form Solid
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Vivien C Abad, et al. Insomnia in Elderly Patients: Recommendations for Pharmacological Management

[2] Jae-Eun Kang, et al. Amyloid-beta dynamics are regulated by orexin and the sleep-wake cycle

[3] David N Neubauer. Almorexant, a dual orexin receptor antagonist for the treatment of insomnia

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Keywords: Almorexant, ACT-078573 supplier, OX Receptor, inhibitors, activators

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