A κ-opioid receptor antagonist
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Aticaprant

Item No. 35464

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[[(2S)-2-(3,5-dimethylphenyl)-1-pyrrolidinyl]methyl]phenoxy]-3-fluoro-benzamide
CAS Number
1174130-61-0
Synonyms
  • CERC-501
  • JNJ-67953964
  • LY2456302
Molecular Formula
C26H27FN2O2
Formula Weight
418.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 5 mg/mlEthanol: 3 mg/ml
SMILES
NC(C1=CC(F)=C(C=C1)OC(C=C2)=CC=C2CN3CCC[C@H]3C4=CC(C)=CC(C)=C4)=O
InChi Code
InChI=1S/C26H27FN2O2/c1-17-12-18(2)14-21(13-17)24-4-3-11-29(24)16-19-5-8-22(9-6-19)31-25-10-7-20(26(28)30)15-23(25)27/h5-10,12-15,24H,3-4,11,16H2,1-2H3,(H2,28,30)/t24-/m0/s1
InChi Key
ZHPMYDSXGRRERG-DEOSSOPVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $117

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    10 mg

    $207

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    25 mg

    $461

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    Product Description

    Aticaprant is a κ-opioid receptor (KOR) antagonist (Ki = 0.807 nM).1 It is selective for KOR over the μ- and δ-opioid receptors (Kis = 24 and 155 nM, respectively). Aticaprant reverses U-69593-induced decreases in nocifensive behavior in the formalin test in rats (ED50 = 0.4 mg/kg). It also reverses U-69593-induced disruptions in prepulse inhibition in rats in a dose-dependent manner. Aticaprant (10 mg/kg) reduces immobility time in the forced swim test in mice. It reduces alcohol self-administration and the progressive ratio breakpoint in rats when administered at a dose of 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rorick-Kehn, L.M., Witkin, J.M., Statnick, M.A., et al. LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders. Neuropharmacology 77, 131-144 (2014).