Product Details
| Product Name:
Aticaprant |
CAS No.:
1174130-61-0 |
| Purity:
99.93% |
Supply Ability:
10g |
| Release date:
2025/07/16 |
Product Introduction
Bioactivity
| Name | Aticaprant |
| Description | Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2] |
| Animal Research | Three male cannulated rats are administered a single 1 mg/kg intravenous (IV) and 10 mg/kg oral (PO) dose of Aticaprant 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). Male mice are administered a single 10 mg/kg PO dose of Aticaprant to determine the pharmacokinetic parameters. Plasma samples are collected at 0.5, 1, 2, 4, 8, and 24 h post-dose and analyzed by LCMS/MS to determine the concentrations of Aticaprant. The plasma and brain binding of Aticaprant is determined by equilibrium dialysis at 1 μM [1]. |
| In vitro | Aticaprant(CERC-501) binds with a high affinity to the human kappa opioid receptor with a 30-fold higher affinity over the human mu-opioid receptor and a 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 [1]. |
| In vivo | METHODS: Mice were given Aticaprant(CERC-501) (0.1 to 3 mg/kg, intraperitoneal injection) 30 minutes before the alcohol deprivation effect (ADE) test and naltrexone (0.3 or 1 mg/kg, intraperitoneal injection) 10 minutes before the test to observe the effect of aticaprant on the ADE effect.
RESULTS 0.3 mg/kg of Aticaprant(CERC-501) and 1 mg/kg of naltrexone reduced the ADE alcohol intake of mice at 4 hours. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (238.95 mM), Sonication is recommended.
|
| Keywords | κ-opioid receptor | OpioidReceptor | Opioid Receptor | LY2456302 | LY 2456302 | Inhibitor | inhibit | CERC501 | CERC 501 | Aticaprant |
| Inhibitors Related | Docusate sodium | Bevenopran | Mirtazapine | (-)-Menthol | SCH 221510 | Naltrexone hydrochloride | Progesterone | Meptazinol hydrochloride | Trimebutine | Mianserin hydrochloride | Amentoflavone | Trimebutine maleate |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library | GPCR Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
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Suppliers |
Update time |
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$/ |
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Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States