GLPBio

CERC-501 (Aticaprant)

Catalog No.: GC19229Purity:>99.50%Synonyms: CERC-501, JNJ-67953964, LY2456302
COASDSData Sheet
CERC-501 (CERC-501) هو مناهض لمستقبلات kappa الأفيونية قويًا ومتغلغلًا مركزيًا مع Ki يبلغ 0.807 نانومتر.

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.

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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المراجع (Citations)

لا تتوفر حاليًا مراجع لهذا المنتج. فيما يلي مجموعة مختارة من المنشورات التي تستشهد بمنتجات GlpBio.
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    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
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    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
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    33, 273–287 (2023)
  • Cell Research cover
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    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
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    Cell Research
    31, 1291–1307 (2021)

الوصف (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.

البروتوكول (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.

وثائق المنتج (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

الخصائص الكيميائية (Chemical Properties)

رقم CAS
1174130-61-0
المرادفات
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
الصيغة الجزيئية
C26H27FN2O2
الوزن الجزيئي
418.5
الذوبانية
DMSO : ≥ 100 mg/mL (238.95 mM)
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

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