An OX2R receptor antagonist
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EMPA

Item No. 29446

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide
CAS Number
680590-49-2
Molecular Formula
C23H26N4O4S
Formula Weight
454.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleEthanol: soluble
SMILES
CCN(C(CN(C1=CC=C(OC)N=C1)S(C2=CC=CC=C2C)(=O)=O)=O)CC3=CN=CC=C3
InChi Code
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
InChi Key
KJPHTXTWFHVJIG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $129

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    10 mg

    $205

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    Product Description

    EMPA is an orexin 2 receptor (OX2R) antagonist (Ki = 1.1 nM).1 It is selective for OX2R over OX1R (Ki = 900 nM). EMPA inhibits orexin-A- and orexin-B-induced calcium mobilization (IC50s = 8.8 and 7.9 nM, respectively) and increases orexin-A- and orexin-B-induced inositol phosphate accumulation (EC50s = 1.1 and 2.4 nM, respectively) in CHO(dHFr-) cells expressing recombinant human OX2R. It reduces spontaneous locomotor activity and orexin-B-induced hyperlocomotion in mice when administered at doses ranging between 10 and 300 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Malherbe, P., Borroni, E., Gobbi, L., et al. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor. Br. J. Pharmacol. 156(8), 1326-1341 (2009).