EMPA

Cat. No. 4558

EMPA C23H26N4O4S [680590-49-2]

Price and Availability

For EMPA pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Chemical Name: N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide

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
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
680590-49-2

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.

If you know of a relevant reference for this product please let us know.

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 .

Do you know of a great paper that uses EMPA from Tocris? If so please let us know.

View Related Products by Target

View Related Products by Product Action

Keywords: EMPA, supplier, supplier, orexin, 2, receptor, OX2, antagonists, inhibits, potent, selective, hyperlocomotion, brain, penetrant, Tocris Bioscience, OX2 Receptor Antagonist products

Quick Order

Find multiple products by catalog number

divider line

Peptide Hormone Receptors Product Listing

Peptide Hormone Receptors Product Listing

Our Peptide Hormone Receptors Listing highlights over 200 products for peptide hormone receptors. Request copy or view PDF today.

divider line

GPCR Product Listing

GPCR Product Listing

Highlights over 450 products for GPCRs. Request copy or view PDF today.

divider line

Appetite Modulation

Written by S. Tucci et al

Peptides Involved in Appetite Modulation Scientific Review

Our Peptides Involved in Appetite Modulation review gives an overview of the peptides implicated in appetite regulation and energy homeostasis. View PDF today.

divider line

Twitter Updates

Follow @Tocris on Twitter

Follow us on Twitter!

Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.