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Almorexant

Almorexant

  • CAT Number: I005246
  • CAS Number: 871224-64-5
  • Molecular Formula: C29H31F3N2O3
  • Molecular Weight: 512.56
  • Purity: ≥95%
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<p style=/line-height:25px/>Almorexant(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.<br>IC50 value: 1.3/0.7 nM(OX1/OX2 receptor) [1] [2]<br>Target: Dual OX!/OX2 receptor<br>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].<br>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].</p>

Catalog Number I005246
CAS Number 871224-64-5
Molecular Formula

C29H31F3N2O3

Purity 95%
Target OX Receptor
Solubility 10 mM in DMSO
Storage Desiccate at -20C
IC50 1.3/0.7 nM(OX1/OX2 receptor) [1] [2]
InChI 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
InChIKey DKMACHNQISHMDN-RPLLCQBOSA-N
SMILES O=C(NC)[C@H](N1[C@@H](CCC2=CC=C(C(F)(F)F)C=C2)C3=C(C=C(OC)C(OC)=C3)CC1)C4=CC=CC=C4
Reference

</br>1:Dual Orexin Receptor Antagonist, Almorexant, in Elderly Patients With Primary Insomnia: A Randomized, Controlled Study. Roth T, Black J, Cluydts R, Charef P, Cavallaro M, Kramer F, Zammit G, Walsh J.Sleep. 2017 Feb 1;40(2). doi: 10.1093/sleep/zsw034. PMID: 28364509 </br>2:Dual orexin receptor antagonist, almorexant, in elderly patients with primary insomnia: a randomized, controlled study. Roth T, Black J, Cluydts R, Charef P, Cavallaro M, Kramer F, Zammit G, Walsh J.Sleep. 2016 Oct 10. pii: sp-00223-16. [Epub ahead of print] PMID: 27748238 </br>3:The Dual Hypocretin Receptor Antagonist Almorexant is Permissive for Activation of Wake-Promoting Systems. Parks GS, Warrier DR, Dittrich L, Schwartz MD, Palmerston JB, Neylan TC, Morairty SR, Kilduff TS.Neuropsychopharmacology. 2016 Mar;41(4):1144-55. doi: 10.1038/npp.2015.256. Epub 2015 Aug 20. PMID: 26289145 Free PMC Article</br>4:Pharmacokinetic and pharmacodynamic interactions between almorexant, a dual orexin receptor antagonist, and desipramine. Cruz HG, Hay JL, Hoever P, Alessi F, te Beek ET, van Gerven JM, Dingemanse J.Eur Neuropsychopharmacol. 2014 Aug;24(8):1257-68. doi: 10.1016/j.euroneuro.2014.05.002. Epub 2014 May 13. PMID: 24880753 </br>5:Formulation development for the orexin receptor antagonist almorexant: assessment in two clinical studies. Dingemanse J, Gehin M, Cruz HG, Hoever P.Drug Des Devel Ther. 2014 Apr 28;8:397-403. doi: 10.2147/DDDT.S62118. eCollection 2014. PMID: 24812492 Free PMC Article</br>6:Entry-into-humans study with ACT-462206, a novel dual orexin receptor antagonist, comparing its pharmacodynamics with almorexant. Hoch M, van Gorsel H, van Gerven J, Dingemanse J.J Clin Pharmacol. 2014 Sep;54(9):979-86. doi: 10.1002/jcph.297. Epub 2014 Apr 21. PMID: 24691844 </br>7:Assessment of the abuse liability of a dual orexin receptor antagonist: a crossover study of almorexant and zolpidem in recreational drug users. Cruz HG, Hoever P, Chakraborty B, Schoedel K, Sellers EM, Dingemanse J.CNS Drugs. 2014 Apr;28(4):361-72. doi: 10.1007/s40263-014-0150-x. PMID: 24627301 </br>8:Pharmacokinetic interactions between the orexin receptor antagonist almorexant and the CYP3A4 inhibitors ketoconazole and diltiazem. Dingemanse J, Cruz HG, Gehin M, Hoever P.J Pharm Sci. 2014 May;103(5):1548-56. doi: 10.1002/jps.23916. Epub 2014 Mar 6. PMID: 24604243 </br>9:The hypocretin/orexin antagonist almorexant promotes sleep without impairment of performance in rats. Morairty SR, Wilk AJ, Lincoln WU, Neylan TC, Kilduff TS.Front Neurosci. 2014 Jan 31;8:3. doi: 10.3389/fnins.2014.00003. eCollection 2014. PMID: 24550767 Free PMC Article</br>10:Validation of an LC-MS/MS method for the quantitative determination of the orexin receptor antagonist almorexant and its four primary metabolites in human plasma. Wagner-Redeker W, Finsterwald I, Dingemanse J.J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Mar 1;951-952:96-103. doi: 10.1016/j.jchromb.2014.01.033. Epub 2014 Jan 30. PMID: 24531213

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