An internal standard for the quantification of almorexant
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Unlabeled Version(s)
13638Almorexant (hydrochloride)
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Almorexant-13C-d3

Item No. 29099

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(R)-2-((S)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-(methyl-13C-d3)-2-phenylacetamide
CAS Number
2738376-75-3
Synonyms
  • ACT 078573-13C-d3
Molecular Formula
C28[13C]H28D3F3N2O3
Formula Weight
516.6
Purity
≥98% deuterated forms (d1-d3)
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: solubleDMSO: solubleMethanol: soluble
SMILES
O=C(N[13C]([2H])([2H])[2H])[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/i1+1D3
InChi Key
DKMACHNQISHMDN-AXIKUPSYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $174

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    1 mg

    $329

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    Product Description

    Almorexant-13C-d3 is intended for use as an internal standard for the quantification of almorexant (Item No. 13638) by GC- or LC-MS. 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).