EMPA

Pricing Availability Delivery Time Qty
Cat.No. 4558 - EMPA | C23H26N4O4S | CAS No. 680590-49-2
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)
Datasheet
Citations (1)
Literature

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.45 100
ethanol 22.73 50

Preparing Stock Solutions

The following data is based on the product molecular weight 454.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: supplier orexin 2 receptor OX2 antagonists inhibits potent selective hyperlocomotion brain penetrant OX2 Receptor

1 Citation for EMPA

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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