CERC-501 (Aticaprant)
(Synonyms: CERC-501; LY-2456302) 目录号 : GC19229
CERC-501 (Aticaprant)是一种高效且能穿透中枢神经系统的κ-阿片受体（KOR）拮抗剂，Ki值为0.807nM。
Cas No.:1174130-61-0
Sample solution is provided at 25 µL, 10mM.
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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.
CERC-501 (Aticaprant)是一种高效且能穿透中枢神经系统的κ-阿片受体（KOR）拮抗剂，Ki值为0.807nM[1]。KOR是一种抑制性G蛋白偶联受体，介导应激、负性情绪及成瘾行为中的负向强化[2]。CERC-501主要用于抑郁症、物质使用障碍及奖赏机制的研究[3][4][5]。
在体内实验中，CERC-501（10mg/kg；口服；60分钟）可逆转慢性尼古丁戒断诱导的雄性ICR小鼠痛觉过敏和焦虑样行为[6]。CERC-501（10mg/kg/天；腹腔注射；连续11天）可逆转雄性C57BL/6J小鼠不可预测慢性轻度应激诱导的快感缺失，恢复蔗糖偏好并提高筑巢评分[7]。
| 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: | |
| Cas No. | 1174130-61-0 | SDF | |
| 别名 | CERC-501; LY-2456302 | ||
| Canonical 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 | ||
| 分子式 | C26H27FN2O2 | 分子量 | 418.5 |
| 溶解度 | DMSO : ≥ 100 mg/mL (238.95 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3895 mL | 11.9474 mL | 23.8949 mL |
| 5 mM | 477.9 μL | 2.3895 mL | 4.779 mL |
| 10 mM | 238.9 μL | 1.1947 mL | 2.3895 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet