EMPA

• Supplier: Tocris Bioscience
• Catalog: 3811
• Prices: $209.00, $879.00
• Sizes: 10 mg, 50 mg
• Function Type: Antagonist
• Cas Number: 680590-49-2
• Chemical Name: N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide
• Formula: C23H26N4O4S
• Molecular Weight: 454.54
• Purity: >98 %
• Description: Highly potent, selective OX 2 receptor antagonist (IC 50 values are 2.3 nM and 1900 nM for OX 2 and OX 1 respectively). Displays negligible or no inhibition of a panel of 80 receptors. Blocks orexin-B- and orexin-A-invoked calcium mobilization in hOX 2 -expressing CHO cells (IC 50 values are 7.9 nM and 8.8 nM respectively); reverses orexin-B-induced hyperlocomotion in mice. Brain penetrant.

Product References

Biochemical and behavioural characterization of EMPA, a novel high-affinity, - Biochemical and behavioural characterization of EMPA, a novel high-affinity,

Malherbe P, Borroni E, Gobbi L, Knust H, Nettekoven M, Pinard E, Roche O, Rogers-Evans M, Wettstein JG, Moreau JL. Br J Pharmacol. 2009 Apr;156(8):1326-41.

Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and - Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and

Malherbe P, Roche O, Marcuz A, Kratzeisen C, Wettstein JG, Bissantz C. Mol Pharmacol. 2010 Jul;78(1):81-93.

Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in - Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in

Mochizuki T, Arrigoni E, Marcus JN, Clark EL, Yamamoto M, Honer M, Borroni E, Lowell BB, Elmquist JK, Scammell TE. Proc Natl Acad Sci U S A. 2011 Mar 15;108(11):4471-6. doi: