
簡要描述:Rufinamide 106308-44-5Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
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| 品牌 | absin | CAS | 106308-44-5 |
|---|---|---|---|
| 分子式 | C10H8F2N4O | 純度 | >98% |
| 分子量 | 238.19 | 貨號 | abs47028065 |
| 規(guī)格 | 10mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | used an anticonvulsant medication | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
Rufinamide 106308-44-5
| 產(chǎn)品描述 | |
| 描述 | Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication. |
| 純度 | >98% |
| 儲存/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 | |
| 別名 | 盧非酰胺;CGP 33101;E 2080;RUF 331 |
| 外觀 | 白色粉末 |
| 可溶性/溶解性 | DMSO : 47 mg/mL (197.32 mM), warmed |
| 生物活性 | |
| 靶點 | Sodium channel |
| In vitro(體外研究) | 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(體內(nèi)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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| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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