Home GPCR & G Protein OX Receptor antagonist Almorexant HCl For research use only.

Almorexant HCl

Synonyms: ACT-078573 HCl

Almorexant HCl (ACT-078573) 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.

Almorexant HCl Chemical Structure

Almorexant HCl Chemical Structure

CAS No. 913358-93-7

Purity & Quality Control

Almorexant HCl Related Products

Signaling Pathway

OX Receptor Signaling Pathways

OX Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO Function assay 30 mins Displacement of [125I]-Orexin A from human OX2R expressed in CHO cells after 30 mins by topcount analysis, Ki = 0.0047 μM. 25267004
CHO Function assay Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release, IC50 = 0.008 μM. 26317591
CHO Function assay Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay, IC50 = 0.008 μM. 23719231
CHO Function assay Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release, IC50 = 0.013 μM. 26317591
CHO Function assay Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay, IC50 = 0.013 μM. 23719231
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Biological Activity

Description Almorexant HCl (ACT-078573) 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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot PhosphoTyr / SHP2 29467942
Growth inhibition assay Tumor volume 29467942
IHC OX1R / Activated caspase-3 H&E staining 29467942
Immunofluorescence BDNF / NPY NPY / ORX-A 32066707
Representative autoradiograms LC / TMN / DRN 22768296
In Vivo
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]
Animal Research Animal Models Wistar rats.
Dosages ~300 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 549.02 Formula

C29H32ClF3N2O3
CAS No. 913358-93-7 SDF Download Almorexant HCl SDF
Smiles CNC(=O)C(C1=CC=CC=C1)N2CCC3=CC(=C(C=C3C2CCC4=CC=C(C=C4)C(F)(F)F)OC)OC.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (131.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 51 mg/mL

Water : Insoluble


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In vivo
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