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Aticaprant

Chemical Structure : Aticaprant

CAS No.: 1174130-61-0

Aticaprant (CERC-501, JSPA 0658, LY2456302)

Catalog No.: PC-62110Not For Human Use, Lab Use Only.

LY 2456302 (CERC-501, JSPA 0658, Aticaprant) is a potent, selective, short-acting antagonist of κ-opioid receptor (KOR) with Ki of 0.81 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LY 2456302 (CERC-501, JSPA 0658, Aticaprant) is a potent, selective, short-acting antagonist of κ-opioid receptor (KOR) with Ki of 0.81 nM.
LY 2456302 (CERC-501, JSPA 0658, Aticaprant) displays >30-fold selectivity over MOR and DOR.
LY 2456302 (CERC-501, JSPA 0658, Aticaprant) selectively and potently occupies central kappa opioid receptors in vivo (ED50=0.33 mg/kg).
LY 2456302 (CERC-501, JSPA 0658, Aticaprant) produces antidepressant-like effects in the mouse forced swim test and enhanced the effects of imipramine and citalopram.
LY 2456302 (CERC-501, JSPA 0658, Aticaprant) shows orally-bioavailablilty and excellent pharmacokinetic properties.

Physicochemical Properties

M.Wt 418.512
Formula C26H27FN2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(4-(((2S)-2-(3,5-dimethylphenyl)-1-pyrrolidinyl)methyl)phenoxy)-3-fluoro-benzamide

References

1. Rorick-Kehn LM, et al. Neuropharmacology. 2014 Feb;77:131-44.

2. Jackson KJ, et al. Neuropharmacology. 2015 Oct;97:270-4.

3. Naganawa M, et al. J Pharmacol Exp Ther. 2016 Feb;356(2):260-6.

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