An antagonist of NPY receptor Y5
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Lu AA33810

Item No. 32913

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide
CAS Number
304008-29-5
Molecular Formula
C19H25N3O2S3
Formula Weight
423.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mM
λmax
225, 244, 255, 363 nm
SMILES
CS(NC[C@@H](CC1)CC[C@H]1NC2=NC3=C(S2)CCSC4=CC=CC=C34)(=O)=O
InChi Code
InChI=1S/C19H25N3O2S3/c1-27(23,24)20-12-13-6-8-14(9-7-13)21-19-22-18-15-4-2-3-5-16(15)25-11-10-17(18)26-19/h2-5,13-14,20H,6-12H2,1H3,(H,21,22)/t13-,14-
InChi Key
UWSBTSAJZMIHBL-HDJSIYSDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $55

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    5 mg

    $206

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    10 mg

    $385

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    25 mg

    $825

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    Product Description

    Lu AA33810 is an antagonist of neuropeptide Y (NPY) receptor Y5 (Ki = 1.5 nM for the human receptor).1 It is selective for Y5 over Y1, Y2, and Y4 (Kis = >10 µM for all in HEK293 membranes expressing rat receptors). Lu AA33810 also binds the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2B (Kis = 478 and 247 nM, respectively). It inhibits NPY-induced calcium mobilization and cAMP accumulation in COS-7 and HEK293 cells expressing the rat Y5 receptor, respectively, in a concentration-dependent manner. Lu AA33810 (10 mg/kg) increases social interaction time in a social exploration test, as well as decreases immobility time in the forced swim test, in rats, indicating anxiolytic- and antidepressant-like activities, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Walker, M.W., Wolinsky, T.D., Jubian, V., et al. The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity. J. Pharmacol. Exp. Ther. 328(3), 900-911 (2009).