A κ-opioid receptor antagonist
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LY2795050

Item No. 33604

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-chloro-4-[4-[[(2S)-2-(3-pyridinyl)-1-pyrrolidinyl]methyl]phenoxy]-benzamide
CAS Number
1346133-08-1
Molecular Formula
C23H22ClN3O2
Formula Weight
407.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
NC(C1=CC(Cl)=C(OC2=CC=C(CN3CCC[C@H]3C4=CN=CC=C4)C=C2)C=C1)=O
InChi Code
InChI=1S/C23H22ClN3O2/c24-20-13-17(23(25)28)7-10-22(20)29-19-8-5-16(6-9-19)15-27-12-2-4-21(27)18-3-1-11-26-14-18/h1,3,5-11,13-14,21H,2,4,12,15H2,(H2,25,28)/t21-/m0/s1
InChi Key
LOOCZNLSXJHWTG-NRFANRHFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $81

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    5 mg

    $180

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    10 mg

    $317

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    25 mg

    $690

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    Product Description

    LY2795050 is a κ-opioid receptor antagonist (Ki = 0.722 nM).1 It is selective for κ-opioid receptors over μ- and δ-opioid receptors (Kis = 25.8 and 153 nM, respectively). LY2795050 (0.1 mg/kg, i.p.) reduces immobility time in the forced swim test, as well as reduces salvinorin A-induced decreases in grooming time in the splash test, indicating antidepressant-like activity, in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mitch, C.H., Quimby, S.J., Diaz, N., et al. Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: Application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. J. Med. Chem. 54(23), 8000-8012 (2011).

    2. Butelman, E.R., McElroy, B.D., Prisinzano, T.E., et al. Impact of pharmacological manipulation of the κ-opioid receptor system on self-grooming and anhedonic-like behaviors in male mice. J. Pharmacol. Exp. Ther. 370(1), 1-8 (2019).