1. GPCR/G Protein
  2. Orexin Receptor (OX Receptor)

Almorexant hydrochloride (Synonyms: ACT-078573 hydrochloride)

Cat. No.: HY-10805A Purity: 99.88%
Handling Instructions

Almorexant Hcl (ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

For research use only. We do not sell to patients.
Almorexant hydrochloride Chemical Structure

Almorexant hydrochloride Chemical Structure

CAS No. : 913358-93-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 174 In-stock
5 mg USD 144 In-stock
10 mg USD 240 In-stock
50 mg USD 828 In-stock
100 mg USD 1440 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Almorexant hydrochloride:

    Almorexant hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2018 Jan 9;9(6):6952-6967.

    Orexin-A and Almorexant promote tyrosine phosphorylation of SHP2/OX1R complex
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    Almorexant Hcl (ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

    IC50 & Target

    IC50 value: 1.3/0.7 nM(OX1/OX2 receptor) [1] [2]

    In Vitro

    [(3)H]Almorexant bound to a single saturable site on hOX(1) and hOX(2) with high affinity (K(d) of 1.3 and 0.17 nM, respectively. In Schild analyses using the [(3)H]inositol phosphates assay, almorexant acted as a competitive antagonist at hOX(1) and as a noncompetitive-like antagonist at hOX(2). In binding kinetic analyses, [(3)H]almorexant had fast association and dissociation rates at hOX(1), whereas it had a fast association rate and a remarkably slow dissociation rate at hOX(2) [1]. in vivo: During the 12-h dark period after dosing, ALM(Almorexant) exacerbated cataplexy in TG mice and increased nonrapid eye movement sleep with heightened sleep/wake fragmentation in both genotypes. ALM showed greater hypnotic potency in WT mice than in TG mice. The 100 mg/kg dose conferred maximal promotion of cataplexy in TG mice and maximal promotion of REM sleep in WT mice. In TG mice, ALM (30 mg/ kg) paradoxically induced a transient increase in active wakefulness [3]. Almorexant 200 mg showed significantly less 'Drug Liking' than both zolpidem doses (p < 0.01), and almorexant 400 mg had smaller effects than zolpidem 20 mg (p < 0.05), while almorexant 1,000 mg was not different from either zolpidem dose [4].

    Clinical Trial
    Molecular Weight




    CAS No.



    CNC([[email protected]@H](C1=CC=CC=C1)N2CCC3=CC(OC)=C(OC)C=C3[[email protected]@H]2CCC4=CC=C(C(F)(F)F)C=C4)=O.Cl

    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 46 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.88%

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