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Aticaprant
Catalog No. TQ0082Cas No. 1174130-61-0
Alias LY-2456302, CERC-501
Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2]
Aticaprant
Catalog No. TQ0082Alias LY-2456302, CERC-501Cas No. 1174130-61-0
Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2]
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $34 | In Stock | |
| 2 mg | $48 | In Stock | |
| 5 mg | $80 | In Stock | |
| 10 mg | $128 | In Stock | |
| 25 mg | $272 | In Stock | |
| 50 mg | $428 | In Stock | |
| 100 mg | $639 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $89 | In Stock |
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Purity:99.93%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2] |
| Targets&IC50 | κ opioid:0.807 nM (Ki) |
| 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] |
| 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]. |
| Alias | LY-2456302, CERC-501 |
| Molecular Weight | 418.5 |
| Formula | C26H27FN2O2 |
| Cas No. | 1174130-61-0 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (238.95 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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