GLPBio

CERC-501 (Aticaprant)

Catalog No.: GC19229Purity:>99.50%Synonyms: CERC-501, JNJ-67953964, LY2456302
COASDSData Sheet
CERC-501 (Aticaprant) is a potent and centrally-penetrant kappa opioid(KOR) receptor antagonist with a Ki of 0.807nM.

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CERC-501 (Aticaprant)
Cas No.: 1174130-61-0
10mM (in 1mL DMSO)In Stock
$69.00
1
5mgIn Stock
$63.00
1
10mgIn Stock
$98.00
1
25mgIn Stock
$166.00
1
50mgIn Stock
$266.00
1
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Description

CERC-501 (Aticaprant) is a potent and centrally-penetrant kappa opioid(KOR) receptor antagonist with a Ki of 0.807nM[1]. KOR is an inhibitory G protein coupled receptor that mediates stress, negative affect, and negative reinforcement in addiction-related behaviors[2]. CERC-501 is primarily used for research into depression, substance-use disorders, and reward mechanisms[3][4][5].

In vivo, CERC-501 (10mg/kg; p.o.; 60min) reversed chronic-nicotine-withdrawal-induced hyperalgesia and anxiety-like behavior in male ICR mice[6]. CERC-501 (10mg/kg/day; i.p.; 11 days) reversed unpredictable chronic mild stress-induced anhedonia, restored sucrose preference and increased nest building scores in male C57BL/6J mice[7].

References:
[1] Rorick-Kehn LM, Witkin JM, Statnick MA, 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. 2014;77:131-144.
[2] Cayir S, Zhornitsky S, Barzegary A, et al. A review of the kappa opioid receptor system in opioid use. Neurosci Biobehav Rev. 2024;162:105713.
[3] Serretti A. Anhedonia: Current and future treatments. PCN Rep. 2025;4(1):e70088. Published 2025 Mar 23.
[4] Hampsey E, Jelen L, Young AH. Aticaprant: (a κ-opioid receptor antagonist) for major depressive disorder. Expert Opin Emerg Drugs. 2024;29(3):193-204.
[5] Krystal AD, Pizzagalli DA, Smoski M, et al. A randomized proof-of-mechanism trial applying the 'fast-fail' approach to evaluating κ-opioid antagonism as a treatment for anhedonia. Nat Med. 2020;26(5):760-768.
[6] Jackson KJ, Jackson A, Carroll FI, Damaj MI. Effects of orally-bioavailable short-acting kappa opioid receptor-selective antagonist LY2456302 on nicotine withdrawal in mice. Neuropharmacology. 2015;97:270-274.
[7] Jacobson ML, Wulf HA, Browne CA, Lucki I. The kappa opioid receptor antagonist aticaprant reverses behavioral effects from unpredictable chronic mild stress in male mice. Psychopharmacology (Berl). 2020;237(12):3715-3728.

Protocol

Animal experiment [1]:

Animal models

male ICR mice

Preparation Method

Naïve male 8-10 week-old ICR mice were housed five per cage in a 21°C humidity controlled facility with ad libitum access to food and water. To assess the effects of acute CERC-501 administration on spontaneous withdrawal from nicotine, mice were infused with nicotine or saline for 14 days. On day 14, mice were anesthetized under isoflurane anesthesia and minipumps were removed in the evening. No analgesic was given after mini pump removal, as this would interfere with hyperalgesia testing. Mice were habituated to the gavage procedure for oral drug administration for 3 days prior to mini pump removal. On day 15, 18-24h after mini pump removal, these mice were pretreated orally (p.o.) 60min prior to testing with either vehicle or CERC-501 (10mg/kg; p.o.). Immediately following the 60min pre-treatment, mice were observed for physical and affective nicotine withdrawal signs.

Dosage form

10mg/kg; p.o.; 60min

Applications

CERC-501 reversed chronic-nicotine-withdrawal-induced hyperalgesia and anxiety-like behavior in male ICR mice.

References:
[1] Jackson KJ, Jackson A, Carroll FI, Damaj MI. Effects of orally-bioavailable short-acting kappa opioid receptor-selective antagonist LY2456302 on nicotine withdrawal in mice. Neuropharmacology. 2015;97:270-274.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1174130-61-0
Synonyms
CERC-501, JNJ-67953964, LY2456302
SMILES
O=C(N)C1=CC=C(OC2=CC=C(CN3[C@H](C4=CC(C)=CC(C)=C4)CCC3)C=C2)C(F)=C1
Molecular Formula
C26H27FN2O2
Molecular Weight
418.5
Solubility
DMSO : ≥ 100 mg/mL (238.95 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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