Aticaprant
Based on 10 publication(s) in Google Scholar
Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
For research use only. We do not sell to patients.
- Purity: 99.59%
- CAS No.: 1174130-61-0
- Formula: C26H27FN2O2
- Molecular Weight:418.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Aticaprant
More- Nat Commun. 2024 Sep 20;15(1):8118. [Abstract]
- Neuron. 2022 Dec 21;110(24):4125-4143.e6. [Abstract]
- Nat Chem Biol. 2025 Jul;21(7):1046-1057. [Abstract]
- Nat Struct Mol Biol. 2026 Jun 22. [Abstract]
- Neuropharmacology. 2020 Feb:163:107726. [Abstract]
- J Neurosci. 2021 Nov 24;41(47):9827-9843. [Abstract]
- Res Sq. 2026 Mar 31:rs.3.rs-9103509. [Abstract]
- bioRxiv. 2025 Oct 24.
- bioRxiv. 2025 January 11.
- bioRxiv. 2024 Feb 6:2024.02.05.578840. [Abstract]
All Opioid Receptor Isoforms
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Biological Activity
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κ Opioid Receptor/KOR |
Aticaprant (CERC-501) binds with high affinity to the human kappa opioid receptor with a 30-fold higher affinity over the human mu opioid receptor and 190-fold higher affinity over the human delta opioid receptor. Aticaprant (CERC-501) shows no appreciable affinity for several non-opioid cell surface G-protein-coupled receptor targets, including monoaminergic, muscarinic, cholinergic, and adrenergic receptors or ion channel/transporter binding targets or the central benzodiazepine binding site[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1174130-61-0
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Appearance Solid
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Molecular Weight 418.50
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Formula C26H27FN2O2
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Color White to off-white
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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
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Synonyms
CERC-501; LY-2456302
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Nat Commun
2024 Sep 20;15(1):8118. PMID: 39304653 -
Neuron
Modulation of 5-HT release by dynorphin mediates social deficits during opioid withdrawal. [Abstract]2022 Dec 21;110(24):4125-4143.e6. PMID: 36202097 -
Nat Chem Biol
2025 Jul;21(7):1046-1057. PMID: 39775170 -
Nat Struct Mol Biol
2026 Jun 22. PMID: 42332075 -
Neuropharmacology
Sex differences in kappa opioid receptor inhibition of latent postoperative pain sensitization in dorsal horn. [Abstract]2020 Feb:163:107726. PMID: 31351975 -
J Neurosci
Sex Differences in Protein Kinase A Signaling of the Latent Postoperative Pain Sensitization That Is Masked by Kappa Opioid Receptors in the Spinal Cord. [Abstract]2021 Nov 24;41(47):9827-9843. PMID: 34531285 -
Res Sq
Oxa-noribogaine reduces alcohol drinking through aversion learning and by altering glutamatergic activity in the mPFC. [Abstract]2026 Mar 31:rs.3.rs-9103509. PMID: 41960323 -
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bioRxiv
Kappa Opioid Receptors Negatively Regulate Real Time Spontaneous Dopamine Signals by Reducing Release and Increasing Uptake. [Abstract]2024 Feb 6:2024.02.05.578840. PMID: 38370660
Solvent & Solubility
DMSO : ≥ 100 mg/mL (238.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.97 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Rats: Three male cannulated rats are administered a single 1 mg/kg intravenous (IV) and 10 mg/kg oral (PO) dose of Aticaprant (CERC-501) to determine the pharmacokinetic parameters. Plasma samples are collected at 0.08 (IV only), 0.25, 0.5, 1, 2, 4, 8, 12 and 24 h post-dose and analyzed by liquid chromatography coupled to tandem mass spectral detection to determine the concentrations of Aticaprant (CERC-501)[1].
Mice: Male mice are administered a single 10 mg/kg PO dose of Aticaprant (CERC-501) to determine the pharmacokinetic parameters. Plasma samples are collected at 0.5, 1, 2, 4, 8, and 24 h post-dose and analyzed by LCeMS/MS to determine the concentrations of Aticaprant (CERC-501). The plasma and brain binding of Aticaprant (CERC-501) is determined by equilibrium dialysis at 1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Rorick-Kehn LM, 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 Feb;77:131-44. [Content Brief]
[2]. Jackson KJ, et al. Effects of orally-bioavailable short-acting kappa opioid receptor-selective antagonist LY2456302on nicotine withdrawal in mice. Neuropharmacology. 2015 Oct;97:270-4. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3895 mL | 11.9474 mL | 23.8949 mL | 59.7372 mL |
| 5 mM | 0.4779 mL | 2.3895 mL | 4.7790 mL | 11.9474 mL | |
| 10 mM | 0.2389 mL | 1.1947 mL | 2.3895 mL | 5.9737 mL | |
| 15 mM | 0.1593 mL | 0.7965 mL | 1.5930 mL | 3.9825 mL | |
| 20 mM | 0.1195 mL | 0.5974 mL | 1.1947 mL | 2.9869 mL | |
| 25 mM | 0.0956 mL | 0.4779 mL | 0.9558 mL | 2.3895 mL | |
| 30 mM | 0.0796 mL | 0.3982 mL | 0.7965 mL | 1.9912 mL | |
| 40 mM | 0.0597 mL | 0.2987 mL | 0.5974 mL | 1.4934 mL | |
| 50 mM | 0.0478 mL | 0.2389 mL | 0.4779 mL | 1.1947 mL | |
| 60 mM | 0.0398 mL | 0.1991 mL | 0.3982 mL | 0.9956 mL | |
| 80 mM | 0.0299 mL | 0.1493 mL | 0.2987 mL | 0.7467 mL | |
| 100 mM | 0.0239 mL | 0.1195 mL | 0.2389 mL | 0.5974 mL |
Aticaprant Related Classifications
HY-101718 Related Classifications
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