Almorexant HCl

Catalog No.S2160

Almorexant HCl Chemical Structure

Molecular Weight(MW): 549.02

Almorexant HCl is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3.

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  • (C) No significant changes were observed compared with PBS control (n = 5) when sSNA is measured as % range. Grouped data for the % range from every treatment group are compared. AXT at 75 mg/kg (n = 4) produced no effect on baseline sympathetic activity. (D) AXT at 30 mg/kg (n = 5) and 75 mg/kg (n = 5) attenuated the effect of intermittent orexin-A (10 pmol×10; n = 5) on sSNA. Statistical significance was determined using one-way analysis of variance followed by Holm-Sidak correction to compare the effects with the control. Data are expressed as mean±S.E.M. ****P<0.0001; ***P<0.001; *P <0.05. #P<0.05 compared with intermittent orexin-A (10 pmol×10).

    J Pharmacol Exp Ther, 2016, 358(3):492-501. . Almorexant HCl purchased from Selleck.

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Biological Activity

Description Almorexant HCl is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3.
Features Orally bioavailable orexin receptor antagonist that has been tested in Phase III clinical trials for treatment of Insomnia.
Targets
OX2 receptor [1] OX1 receptor [1]
3.4 nM 6.6 nM
In vitro

Almorexant inhibits the increase in intracellular Ca2+ induced by 10 nM human orexin-A in Chinese hamster ovary cells with IC50 of 16 nM (rat) and 13 nM (human) for the OX1 receptor and 15 nM (rat) and 8 nM (human) for the OX2 receptor. [1]

In vivo Almorexant (300 mg/kg p.o.) decreases alertness, and increases electrophysiological indices of both non-REM and REM sleep in male Wistar rats. In dogs, Almorexant (100 mg/kg p.o.) causes somnolence and increases surrogate markers of REM sleep. [1] Almorexant induces a robust antidepressant-like effect and the restoration of stress-related HPA axis defect independently from a neurogenic action. [2] In addition, Almorexant also reduces ethanol self-administration in high-drinking rodent models. [3]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Wistar rats.
  • Formulation: Polyethylene glycol (PEG) 400 or 0.25% methylcellulose in water
  • Dosages: ~300 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 72 mg/mL (131.14 mM)
Ethanol 51 mg/mL (92.89 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+25% β-cyclodextrin in saline
For best results, use promptly after mixing.
9mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 549.02
Formula

C29H32ClF3N2O3

CAS No. 913358-93-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01954589 Completed Safety|Tolerability|Pharmacodynamics|Pharmacokinetics Idorsia Pharmaceuticals Ltd. November 2011 Phase 1
NCT01954589 Completed Safety|Tolerability|Pharmacodynamics|Pharmacokinetics Idorsia Pharmaceuticals Ltd. November 2011 Phase 1
NCT01243060 Completed Healthy Volunteers Northern California Institute of Research and Education|U.S. Army Medical Research and Materiel Command May 2011 Not Applicable
NCT01243060 Completed Healthy Volunteers Northern California Institute of Research and Education|U.S. Army Medical Research and Materiel Command May 2011 Not Applicable
NCT01987739 Completed Abuse Potential Study Midnight Pharma LLC September 2009 Phase 1
NCT01987739 Completed Abuse Potential Study Midnight Pharma LLC September 2009 Phase 1

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OX Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID