For research use only. Not for therapeutic Use.
EMPA(CAT: R042203) is a high-affinity, selective, and reversible orexin OX₂ receptor antagonist. It binds to human and rat OX₂ receptors with Kd values of 1.1 nM and 1.4 nM, respectively, and competitively blocks orexin-A and orexin-B signaling with pA₂ values of 8.6 and 8.8. In cellular assays, EMPA inhibits orexin-induced [Ca²⁺]i responses with IC₅₀ values around 8 nM, demonstrating potent receptor antagonism. In vivo, EMPA dose-dependently reverses orexin-B–induced hyperlocomotion and reduces spontaneous locomotor activity in mice and rats without nonspecific behavioral suppression. EMPA is a valuable tool for exploring orexin receptor biology, sleep-wake regulation, and neuropsychiatric disease mechanisms.
CAS Number | 680590-49-2 |
Synonyms | N-ethyl-2-[(6-methoxypyridin-3-yl)-(2-methylphenyl)sulfonylamino]-N-(pyridin-3-ylmethyl)acetamide |
Molecular Formula | C23H26N4O4S |
Purity | ≥95% |
IUPAC Name | N-ethyl-2-[(6-methoxypyridin-3-yl)-(2-methylphenyl)sulfonylamino]-N-(pyridin-3-ylmethyl)acetamide |
InChI | InChI=1S/C23H26N4O4S/c1-4-26(16-19-9-7-13-24-14-19)23(28)17-27(20-11-12-22(31-3)25-15-20)32(29,30)21-10-6-5-8-18(21)2/h5-15H,4,16-17H2,1-3H3 |
InChIKey | KJPHTXTWFHVJIG-UHFFFAOYSA-N |
SMILES | CCN(CC1=CN=CC=C1)C(=O)CN(C2=CN=C(C=C2)OC)S(=O)(=O)C3=CC=CC=C3C |
Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |