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Chemical Structure : LY 2456302
CAS No.: 1174130-61-0
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $528 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 418.512 | |
| Formula | C26H27FN2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-(4-(((2S)-2-(3,5-dimethylphenyl)-1-pyrrolidinyl)methyl)phenoxy)-3-fluoro-benzamide |
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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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