Catalog Number: 4558
Chemical Name: N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide
Biological Activity
Highly potent, selective OX2 receptor antagonist (IC50 values are 2.3 nM and 1900 nM for OX2 and OX1 respectively). Displays negligible or no inhibition of a panel of 80 receptors. Blocks orexin-B- and orexin-A-invoked calcium mobilization in hOX2-expressing CHO cells (IC50 values are 7.9 nM and 8.8 nM respectively); reverses orexin-B-induced hyperlocomotion in mice. Brain penetrant.
Technical Data
  • M.Wt:
    454.54
  • Formula:
    C23H26N4O4S
  • Solubility:
    Soluble to 100 mM in DMSO and to 50 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    680590-49-2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor.
    Malherbe et al.
    Br.J.Pharmacol., 2009;156:1326
  2. Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in narcoleptic mice.
    Mochizuki et al.
    Proc.Natl.Acad.Sci.U.S.A, 2011;108:4471
  3. Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and orexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-
    Malherbe et al.
    Mol.Pharmacol., 2010;78:81
Citations:

The citations listed below are publications that use Tocris products. Selected citations for EMPA include:

2 Citations: Showing 1 - 2
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  1. The sleep-modulating peptide orexin-B protects midbrain dopamine neurons from degeneration, alone or in cooperation with nicotine.
    Authors: Guerreiro Et al.
    Mol.Pharmacol. 2015;87:525
  2. Both Ox1R and Ox2R orexin receptors contribute to the cardiorespiratory response evoked from the perifornical hypothalamus.
    Authors: Beig Et al.
    Clin.Exp.Pharmacol.Physiol. 2015;42:1059

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