Product Details
| Product Name:
Opicapone |
CAS No.:
923287-50-7 |
| Purity:
99.36% |
Supply Ability:
10g |
| Release date:
2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | Opicapone |
| 描述 | Opicapone (BIA 9-1067) reduces the ATP content of the cells (IC50: 98 μM). Opicapone is an effective third-generation catechol-O-methyltransferase inhibitor for the research of Parkinson's disease and motor fluctuations. |
| 體外活性 | Opicapone decreases the mitochondrial membrane potential of the cells (IC50: 181 μM). Opicapone has a prolonged inhibitory effect on peripheral COMT, which extends the bioavailability of L-DOPA, without inducing toxicity. Incubation of human primary hepatocytes for 24 h with increasing concentrations of Ro 40-7592, OR-611 or Opicapone resulted in a concentration-dependent decrease in the mitochondrial membrane potential of the cells, evaluated by the ratio JC-1 aggregates over JC-1 monomer (ratio λex 544 λem 590 over λex 485 λem 538) [1]. |
| 體內(nèi)活性 | Opicapone inhibited rat peripheral COMT with ED50 values below 1.4 mg kg(-1) up to 6 h post-administration.?The effect was sustained over the first 8 h and by 24 h COMT had not returned to control values.?A single administration of opicapone resulted in increased and sustained plasma levodopa levels with a concomitant reduction in 3-O-methyldopa from 2 h up to 24 h post-administration, while tolcapone produced significant effects only at 2 h post-administration.?The effects of opicapone on brain catecholamines after levodopa administration were sustained up to 24 h post-administration.?Opicapone was also the least potent compound in decreasing both the mitochondrial membrane potential and the ATP content in human primary hepatocytes after a 24 h incubation period[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 (242.03 mM), Sonication is recommended.
|
| 關(guān)鍵字 | Inhibitor | inhibit | COMT | Opicapone |
| 相關(guān)產(chǎn)品 | Serotonin hydrochloride | Risedronate Sodium | Risedronic Acid | 3-Methoxybenzamide | Entacapone | Minodronic acid monohydrate | OU749 | Ibandronate sodium | Testosterone propionate | Alendronate sodium hydrate | Flopropione | (E)-Daporinad |
| 相關(guān)庫(kù) | FDA上市及藥典收錄分子庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 經(jīng)典已知活性庫(kù) | EMA 上市藥物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | FDA 上市藥物庫(kù) | 代謝化合物庫(kù) | 臨床期小分子藥物庫(kù) | 已知活性化合物庫(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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