Cat. No. 4558
Chemical Name: N-Ethyl-2-[(6-methoxy-3-pyridinyl)[
Biological ActivityHighly 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.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Mochizuki et al (2011) Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in narcoleptic mice. Proc.Natl.Acad.Sci.U.S.A 108 4471. PMID: 21368172.
Malherbe et al (2010) 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-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA). Mol.Pharmacol. 78 81. PMID: 20404073.
Malherbe et al (2009) Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor. Br.J.Pharmacol. 156 1326. PMID: 19751316.
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Citations are publications that use Tocris products. Selected citations for EMPA include:
Guerreiro et al (2015) The sleep-modulating peptide orexin-B protects midbrain dopamine neurons from degeneration, alone or in cooperation with nicotine. Mol.Pharmacol. 87 525. PMID: 25552485 .
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Keywords: EMPA, supplier, supplier, orexin, 2, receptor, OX2, antagonists, inhibits, potent, selective, hyperlocomotion, brain, penetrant, Tocris Bioscience, OX2 Receptor Antagonist products