| CAS NO: | 106308-44-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 238.19 |
|---|---|
| Formula | C10H8F2N4O |
| CAS No. | 106308-44-5 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 47 mg/mL (197.3 mM) |
| Water:<1 mg/mL | |
| Ethanol:<1 mg/mL | |
| Other info | Chemical Name: 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide InChi Key: POGQSBRIGCQNEG-UHFFFAOYSA-N InChi Code: InChI=1S/C10H8F2N4O/c11-7-2-1-3-8(12)6(7)4-16-5-9(10(13)17)14-15-16/h1-3,5H,4H2,(H2,13,17) SMILES Code: O=C(C1=CN(CC2=C(F)C=CC=C2F)N=N1)N |
| Synonyms | E-2080; RUF-331; E2080; CGP-33101; RUF331; CGP 33101; E 2080; RUF 331; CGP33101; Trade names: BANZEL; Inovelon. |
| In Vitro | In vitro activity: 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 | 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. |
| Animal model | Dogs |
| Formulation & Dosage | 20 mg/kg; oral |
| References | Int J Clin Pract. 2006 Nov;60(11):1497-501; J Vet Pharmacol Ther. 2012 Dec;35(6):529-33 |
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