An orexin 1 and orexin 2 receptor antagonist
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Labeled Version(s)
29099Almorexant-13C-d3
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Almorexant (hydrochloride)

Item No. 13638

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αR,1S)-3,4-dihydro-6,7-dimethoxy-N-methyl-α-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-2(1H)-isoquinolineacetamide, monohydrochloride
CAS Number
913358-93-7
Synonyms
  • ACT 078573
Molecular Formula
C29H31F3N2O3 • HCl
Formula Weight
549.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.25 mg/mlEthanol: 10 mg/ml
λmax
285 nm
SMILES
O=C(NC)[C@@H](C1=CC=CC=C1)N2CCC3=C(C=C(OC)C(OC)=C3)[C@@H]2CCC4=CC=C(C(F)(F)F)C=C4
InChi Code
InChI=1S/C29H31F3N2O3/c1-33-28(35)27(20-7-5-4-6-8-20)34-16-15-21-17-25(36-2)26(37-3)18-23(21)24(34)14-11-19-9-12-22(13-10-19)29(30,31)32/h4-10,12-13,17-18,24,27H,11,14-16H2,1-3H3,(H,33,35)/t24-,27+/m0/s1
InChi Key
DKMACHNQISHMDN-RPLLCQBOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $213

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    10 mg

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    Product Description

    Almorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 4.7 and 0.9 nM, respectively, in a radioligand binding assay).1 It decreases the latency to persistent non-rapid eye movement (NREM) sleep and increases the duration of NREM and REM sleep in male rats when administered at a dose of 100 mg/kg.2 Almorexant (300 mg/kg) does not impair spatial learning and memory in the Morris water maze and does not reverse spatial memory impairments induced by scopolamine in rats.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Malherbe, P., Borroni, E., Pinard, E., et al. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: Comparison with selective OX1 and OX2 antagonists. Mol. Pharmacol. 76(3), 618-631 (2015).

    2. Brisbare-Roch, C., Dingemanse, J., Koberstein, R., et al. Promotion of sleep by targeting the orexin system in rats, dogs and humans. Nat. Med. 13(2), 150-155 (2007).

    3. Dietrich, H., and Jenck, F. Intact learning and memory in rats following treatment with the dual orexin receptor antagonist almorexant. Psychopharmacology (Berl.) 212(2), 145-154 (2010).