Almorexant-13C,d3

• UNSPSC Description:

  Almorexant-13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) 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, respectively.

• Target Antigen:

  Isotope-Labeled Compounds; Orexin Receptor (OX Receptor)

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

  GPCR/G Protein;Neuronal Signaling;Others

• Field of Research:

  Neurological Disease; Endocrinology

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C([C@H](N1CCC2=C([C@@H]1CCC3=CC=C(C=C3)C(F)(F)F)C=C(C(OC)=C2)OC)C4=CC=CC=C4)N[13C]([2H])([2H])[2H]

• Molecular Weight:

  516.57

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. |[2]Cruz HG, et al. Assessment of the abuse liability of a dual orexin receptor antagonist: a crossover study of almorexant and zolpidem in recreational drug users. CNS Drugs. 2014 Apr;28(4):361-72.|[3]Malherbe P, 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. 2009 Sep;76(3):618-31.|[4]Sifferlen T, et al. Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1539-42.|[5]Black SW, et al. Almorexant promotes sleep and exacerbates cataplexy in a murine model of narcolepsy. Sleep. 2013 Mar 1;36(3):325-36.|[6]Dayot S, et al. In vitro, in vivo and ex vivo demonstration of the antitumoral role of hypocretin-1/orexin-A and almorexant in pancreatic ductal adenocarcinoma. Oncotarget. 2018 Jan 9;9(6):6952-6967.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported