EMPA

Tocris Bioscience, part of Bio-Techne | Catalog # 4558

COA / SDS

Highly potent and selective OX2 antagonist; brain penetrant

Key Product Details

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)
Molecular Weight:	454.54

View Full Technical Details for EMPA

Technical Data
Citations

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 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	2.20 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

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References for EMPA

References are publications that support the biological activity of the 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