EMPA

Key Product Details

Product Description

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.

Product Specifications for EMPA

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.20 mL	11.00 mL	22.00 mL
5 mM	0.44 mL	2.20 mL	4.40 mL
10 mM	0.22 mL	1.10 mL	2.20 mL
50 mM	0.04 mL	0.22 mL	0.44 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 15 publications citing the usage of this product.

• Mochizuki Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in narcoleptic mice. Proc.Natl.Acad.Sci.U.S.A 2011 PMID: 21368172
• Malherbe 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. 2010 PMID: 20404073
• Malherbe Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX₂ receptor. Br.J.Pharmacol. 2009 PMID: 19751316

Product Documents for EMPA