Product Details
| Product Name:
Aticaprant |
CAS No.:
1174130-61-0 |
| Purity:
99.93% |
Supply Ability:
10g |
| Release date:
2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | Aticaprant |
| 描述 | Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2] |
| 動(dòng)物實(shí)驗(yàn) | 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]. |
| 體外活性 | 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]. |
| 體內(nèi)活性 | 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] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 100 mg/mL (238.95 mM)
|
| 關(guān)鍵字 | inhibit | Opioid Receptor | CERC501 | Inhibitor | CERC 501 | Aticaprant | LY2456302 | LY 2456302 |
| 相關(guān)產(chǎn)品 | Docusate sodium | Bevenopran | Mirtazapine | Sinomenine | (-)-Menthol | Matrine | SCH 221510 | Progesterone | Naltrexone hydrochloride | Trimebutine | Mianserin hydrochloride | Amentoflavone |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 疼痛相關(guān)化合物庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 膜蛋白靶向化合物庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | 已知活性化合物庫(kù) | GPCR靶點(diǎn)分子庫(kù) | 抗癌藥物庫(kù) |
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