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Description: Highly potent and selective OX2 antagonist; brain penetrant
Chemical Name: N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide
Purity: ≥98% (HPLC)
Biological Activity for EMPA
EMPA is a 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 for EMPA
| M. Wt | 454.54 |
| Formula | C23H26N4O4S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 680590-49-2 |
| PubChem ID | 9981404 |
| InChI Key | KJPHTXTWFHVJIG-UHFFFAOYSA-N |
| Smiles | O=C(CN(C2=CN=C(OC)C=C2)S(C3=C(C)C=CC=C3)(=O)=O)N(CC)CC1=CN=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for EMPA
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.45 | 100 | |
| ethanol | 22.73 | 50 |
Preparing Stock Solutions for EMPA
The following data is based on the product molecular weight 454.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.2 mL | 11 mL | 22 mL |
| 5 mM | 0.44 mL | 2.2 mL | 4.4 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.2 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets for EMPA
References for EMPA
References are publications that support the biological activity of the product.
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
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- Mol.Pharmacol. 78 81 PMID: 20404073
If you know of a relevant reference for EMPA, please let us know.
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Keywords: EMPA, EMPA supplier, supplier, orexin, 2, receptor, OX2, antagonists, inhibits, potent, selective, hyperlocomotion, brain, penetrant, Receptor, 4558, Tocris Bioscience
4 Citations for EMPA
Citations are publications that use Tocris products. Selected citations for EMPA include:
Jennifer J et al (2021) Orexin receptor antagonists reverse aberrant dopamine neuron activity and related behaviors in a rodent model of stress-induced psychosis. Transl Psychiatry 11 114 PMID: 33558469
Ralph J et al (2020) Orexin signaling in GABAergic lateral habenula neurons modulates aggressive behavior in male mice. Nat Neurosci 23 638-650 PMID: 32284606
Beig et al (2015) Both Ox1R and Ox2R orexin receptors contribute to the cardiorespiratory response evoked from the perifornical hypothalamus. Clin.Exp.Pharmacol.Physiol. 42 1059 PMID: 26174505
Guerreiro et al (2015) The sleep-modulating peptide orexin-B protects midbrain DA neurons from degeneration, alone or in cooperation with nicotine. Mol.Pharmacol. 87 525 PMID: 25552485
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Peptides Involved in Appetite Modulation Scientific Review
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