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      Rufinamide (CGP 33101; RUF 331)
      Rufinamide (CGP 33101; RUF 331)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1643
      CAS #: 106308-44-5Purity ≥98%

      Description: Rufinamide (also known as CGP 33101; E 2080; RUF 331) is a voltage-gated sodium channel blocker and a novel antiepilepic agent. It is a board spectrum anticonvulsant that is used in combination with other medication and therapy to treat Lennox–Gastaut syndrome and various other seizure disorders. Rufinamide has efficacy for partial seizures. Rufinamide prolongs the inactivation of sodium channels and limits the frequency of action potential firing in cultured and acutely isolated neurons.           

      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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      • 香港大学
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      Molecular Weight (MW)238.19
      FormulaC10H8F2N4O
      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; RUF331; E 2080; RUF 331; CGP-33101; CGP 33101; CGP33101; Trade names: BANZEL; Inovelon.


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      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 VivoRufinamide 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 modelDogs
      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

      These protocols are for reference only. InvivoChem does not independently validate these methods.

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