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| 品牌 | absin | CAS | 106308-44-5 |
|---|---|---|---|
| 分子式 | C10H8F2N4O | 纯度 | ＞98% |
| 分子量 | 238.19 | 货号 | abs47028065 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | used an anticonvulsant medication | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Rufinamide 106308-44-5
| 产品描述 | |
| 描述 | Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication. |
| 纯度 | ＞98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 卢非酰胺；CGP 33101；E 2080；RUF 331 |
| 外观 | 白色粉末 |
| 可溶性/溶解性 | DMSO : 47 mg/mL (197.32 mM), warmed |
| 生物活性 | |
| 靶点 | Sodium channel |
| In vitro(体外研究) | Rufinamide is extensively metabolised by non-CYP450 systems with a half-life of 8-12 hours. Rufinamide’s mechanism of action is thought to be inhibition of sodium-dependent action potentials in neurons, with possible membrane-stabilising effects. Rufinamide hydrolysis is mediated primarily by human carboxylesterase (hCE) 1 and is nonsaturable up to 500 μM. |
| In vivo(体内研究) | Rufinamide given orally at 20 mg/kg every 12 h in healthy dogs should result in a plasma concentration and half-life sufficient to achieve the therapeutic level extrapolated from humans without short-term adverse effects in adult dogs. Rufinamide alleviates injury-induced mechanical allodynia for 4 hours. Rufinamide reduces peak current and stabilizes the inactivated state of voltage-gated sodium channel Nav1.7, with similar effects in dorsal root ganglion neurons in the Spared Nerve Injury neuropathic pain model in mice. Rufinamide suppresses pentylenetetrazol-induced seizures in mice (ED(50) 45.8 mg/kg) but not rats, and is active against MES-induced tonic seizures in mice (ED(50) 23.9 mg/kg) and rats (ED(50) 6.1 mg/kg). Rufinamide suppresses pentylenetetrazol-, bicuculline-, and picrotoxin-induced clonus in mice (ED(50) 54.0, 50.5, and 76.3 mg/kg, respectively). Rufinamide is partially effective in the mouse strychnine test. |
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| 研究领域 | |
| 研究领域 | Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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